5-HT受容体
阻害剤の選択性比較
カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
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水 | DMSO | アルコール | ||
S1333 | Fluoxetine HCl | 4 mg/mL | 69 mg/mL | 69 mg/mL |
S2464 | Sevoflurane | ' mg/mL | ||
S1441 | Venlafaxine HCl | 55.5 mg/mL | 55.5 mg/mL | 55.5 mg/mL |
S1869 | Dapoxetine HCl | 68 mg/mL | 68 mg/mL | 68 mg/mL |
S1483 | Iloperidone | <1 mg/mL | 27 mg/mL | 4 mg/mL |
S8021 | Vortioxetine (Lu AA21004) HBr | <1 mg/mL | 76 mg/mL | 17 mg/mL |
S1336 | Fluvoxamine maleate | <1 mg/mL | 87 mg/mL | 87 mg/mL |
S4053 | Sertraline HCl | <1 mg/mL | 69 mg/mL | 15 mg/mL |
S3024 | Lamotrigine | <1 mg/mL | 10 mg/mL | 3 mg/mL |
S2541 | Clomipramine HCl | 70 mg/mL | 70 mg/mL | 70 mg/mL |
S4113 | Desvenlafaxine | <1 mg/mL | 37 mg/mL | 3 mg/mL |
S4064 | Escitalopram Oxalate | 25 mg/mL | 83 mg/mL | <1 mg/mL |
S2084 | Duloxetine HCl | <1 mg/mL | 67 mg/mL | <1 mg/mL |
S3140 | Milnacipran HCl | 57 mg/mL | 57 mg/mL | 57 mg/mL |
S3183 | Amitriptyline HCl | 15 mg/mL | 63 mg/mL | 63 mg/mL |
S5239 | Paroxetine mesylate | -1 mg/mL | 85 mg/mL | -1 mg/mL |
S9239 | Isocorynoxeine | -1 mg/mL | 77 mg/mL | -1 mg/mL |
S3817 | Harmine hydrochloride | 21 mg/mL | 21 mg/mL | -1 mg/mL |
S9258 | (+)-Isocorynoline | -1 mg/mL | 32 mg/mL | -1 mg/mL |
S5693 | Levomilnacipran Hydrochloride | -1 mg/mL | 57 mg/mL | -1 mg/mL |
S1642 | Methyldopa | <1 mg/mL | 2 mg/mL | <1 mg/mL |
S9039 | Albiflorin | -1 mg/mL | 96 mg/mL | -1 mg/mL |
S4749 | Citalopram HBr | 81 mg/mL | 81 mg/mL | '81 mg/mL |
S8183 | Pimavanserin | 100 mg/mL | 100 mg/mL | 100 mg/mL |
S5655 | Venlafaxine | <1 mg/mL | 55 mg/mL | '<1 mg/mL |
S5485 | Desipramine Hydrochloride | -1 mg/mL | 60 mg/mL | -1 mg/mL |
S4112 | Desvenlafaxine Succinate | <1 mg/mL | 80 mg/mL | <1 mg/mL |
S2582 | Trazodone HCl | <1 mg/mL | 4 mg/mL | <1 mg/mL |
S5071 | Duloxetine | ' mg/mL | ||
S4377 | Imipramine HCl | 63 mg/mL | 63 mg/mL | 63 mg/mL |
S9510 | Protriptyline hydrochloride | -1 mg/mL | 60 mg/mL | -1 mg/mL |
S3175 | Atomoxetine HCl | 2 mg/mL | 58 mg/mL | 37 mg/mL |
S5563 | Thioridazine hydrochloride | -1 mg/mL | 81 mg/mL | -1 mg/mL |
S4740 | Sodium ferulate | 43 mg/mL | 2 mg/mL | <1 mg/mL |
S2459 | Clozapine | <1 mg/mL | 65 mg/mL | 32 mg/mL |
S2493 | Olanzapine | <1 mg/mL | 62 mg/mL | 9 mg/mL |
S2232 | Ketanserin | <1 mg/mL | 2 mg/mL | <1 mg/mL |
S1245 | Latrepirdine 2HCl | <1 mg/mL | 24 mg/mL | 13 mg/mL |
S0779 | Pirenperone | <1 mg/mL | 17 mg/mL | 26 mg/mL |
S2649 | SB 200646 | ˂1 mg/mL | 53 mg/mL | 2 mg/mL |
S0476 | SCH-23390 hydrochloride | 20 mg/mL | 65 mg/mL | 25 mg/mL |
S0313 | Volinanserin | ˂1 mg/mL | 75 mg/mL | '75 mg/mL |
S2644 | Lerisetron | <1 mg/mL | 58 mg/mL | 58 mg/mL |
S2698 | RS-127445 | <1 mg/mL | 56 mg/mL | 8 mg/mL |
S1243 | Agomelatine | <1 mg/mL | 48 mg/mL | 48 mg/mL |
S1283 | Asenapine maleate | <1 mg/mL | 80 mg/mL | <1 mg/mL |
S3005 | Paroxetine HCl | 1 mg/mL | 73 mg/mL | ' 35 mg/mL |
S1615 | Risperidone | <1 mg/mL | 4 mg/mL | 4 mg/mL |
S1444 | Ziprasidone HCl | <1 mg/mL | 90 mg/mL | <1 mg/mL |
S2663 | WAY-100635 Maleate | <1 mg/mL | 85 mg/mL | 85 mg/mL |
S2112 | Blonanserin | <1 mg/mL | <1 mg/mL | <1 mg/mL |
S2849 | SB269970 HCl | <1 mg/mL | 11 mg/mL | <1 mg/mL |
S1345 | Granisetron HCl | 69 mg/mL | 1 mg/mL | 1 mg/mL |
S2016 | Mirtazapine | <1 mg/mL | 53 mg/mL | 53 mg/mL |
S2894 | SB742457 | <1 mg/mL | 78 mg/mL | 2 mg/mL |
S2677 | BRL-15572 Dihydrochloride | <1 mg/mL | 96 mg/mL | 40 mg/mL |
S8010 | PRX-08066 Maleic acid | 104 mg/mL | 104 mg/mL | 98 mg/mL |
S1390 | Ondansetron HCl | 24 mg/mL | 66 mg/mL | 10 mg/mL |
S1898 | Tropisetron HCl | 46 mg/mL | 35 mg/mL | <1 mg/mL |
S1394 | Pizotifen Malate | <1 mg/mL | 21 mg/mL | <1 mg/mL |
S2106 | Azasetron HCl | 3 mg/mL | <1 mg/mL | <1 mg/mL |
S4249 | Flopropione | <1 mg/mL | 36 mg/mL | 36 mg/mL |
S4086 | Loxapine Succinate | <1 mg/mL | 89 mg/mL | 2 mg/mL |
S1996 | Ondansetron | <1 mg/mL | 0.1 mg/mL | <1 mg/mL |
S2856 | SB 271046 hydrochloride | <1 mg/mL | 40 mg/mL | <1 mg/mL |
S5326 | Dolasetron | <1 mg/mL | 64 mg/mL | <1 mg/mL |
S5472 | Nafronyl oxalate salt | 94 mg/mL | 94 mg/mL | 94 mg/mL |
S3050 | Palonosetron HCl | 67 mg/mL | <1 mg/mL | <1 mg/mL |
S4889 | Perospirone hydrochloride | -1 mg/mL | 92 mg/mL | '-1 mg/mL |
S5857 | Trazodone | <1 mg/mL | 45 mg/mL | 17 mg/mL |
S3054 | Alverine Citrate | <1 mg/mL | 95 mg/mL | <1 mg/mL |
S2865 | VUF 10166 | <1 mg/mL | 21 mg/mL | 61 mg/mL |
S5398 | Nefazodone hydrochloride | -1 mg/mL | 22 mg/mL | '-1 mg/mL |
S4635 | Cyproheptadine hydrochloride sesquihydrate | <1 mg/mL | 70 mg/mL | 13 mg/mL |
S4748 | Ondansetron Hydrochloride Dihydrate | 73 mg/mL | 73 mg/mL | 40 mg/mL |
S4694 | Alosetron Hydrochloride | 1 mg/mL | <1 mg/mL | <1 mg/mL |
S5714 | lurasidone | <1 mg/mL | 7 mg/mL | <1 mg/mL |
S3706 | Sarpogrelate hydrochloride | 93 mg/mL | 93 mg/mL | 30 mg/mL |
S3723 | Ramosetron Hydrochloride | 63 mg/mL | 63 mg/mL | '1 mg/mL |
S2346 | Puerarin | <1 mg/mL | 86 mg/mL | <1 mg/mL |
S5538 | Tropisetron | 56 mg/mL | 10 mg/mL | -1 mg/mL |
S5428 | Promazine hydrochloride | -1 mg/mL | 64 mg/mL | -1 mg/mL |
S4283 | Cyclobenzaprine HCl | 62 mg/mL | 62 mg/mL | 62 mg/mL |
S5052 | Granisetron | -1 mg/mL | 11 mg/mL | '-1 mg/mL |
S5749 | Chlorpromazine | -1 mg/mL | 64 mg/mL | -1 mg/mL |
S2669 | LY310762 HCl | <1 mg/mL | 0.4 mg/mL | <1 mg/mL |
S9174 | Xanthotoxol | -1 mg/mL | 40 mg/mL | -1 mg/mL |
S5740 | Palonosetron | -1 mg/mL | 59 mg/mL | ''-1 mg/mL |
S5060 | Metadoxine | -1 mg/mL | 59 mg/mL | -1 mg/mL |
S0496 | PF-04995274 | <1 mg/mL | 86 mg/mL | 20 mg/mL |
S0104 | Pardoprunox (SLV-308) hydrochloride | <1 mg/mL | 30 mg/mL | '<1 mg/mL |
S2578 | 1-Phenylbiguanide | 35 mg/mL | 35 mg/mL | '17 mg/mL |
S1436 | Tianeptine sodium | 91 mg/mL | 91 mg/mL | 91 mg/mL |
S1432 | Sumatriptan Succinate | 83 mg/mL | 83 mg/mL | <1 mg/mL |
S2875 | Prucalopride | <1 mg/mL | 60 mg/mL | 38 mg/mL |
S1975 | Aripiprazole | <1 mg/mL | 90 mg/mL | <1 mg/mL |
S1488 | Naratriptan HCl | 22 mg/mL | 74 mg/mL | <1 mg/mL |
S1607 | Rizatriptan Benzoate | 46 mg/mL | 20 mg/mL | <1 mg/mL |
S1649 | Zolmitriptan | <1 mg/mL | 58 mg/mL | 58 mg/mL |
S1385 | Mosapride Citrate | <1 mg/mL | 90 mg/mL | <1 mg/mL |
S3180 | Eletriptan HBr | <1 mg/mL | 93 mg/mL | <1 mg/mL |
S4247 | Prucalopride Succinate | 97 mg/mL | 97 mg/mL | <1 mg/mL |
S4259 | Vilazodone HCl | <1 mg/mL | 96 mg/mL | <1 mg/mL |
S2096 | Almotriptan Malate | <1 mg/mL | 94 mg/mL | 53 mg/mL |
S5741 | Quetiapine | -1 mg/mL | 77 mg/mL | '-1 mg/mL |
S5848 | Frovatriptan Succinate | 72 mg/mL | 72 mg/mL | <1 mg/mL |
S6489 | Lasmiditan succinate | 14 mg/mL | 100 mg/mL | '9 mg/mL |
S5401 | Tegaserod Maleate | <1 mg/mL | 83 mg/mL | 8 mg/mL |
S2852 | BRL-54443 | <1 mg/mL | 46 mg/mL | 2 mg/mL |
S5153 | Tetrahydroberberine | -1 mg/mL | 6 mg/mL | -1 mg/mL |
S5253 | Cisapride | <1 mg/mL | 93 mg/mL | '<1 mg/mL |
S6324 | 5-Methoxytryptamine | -1 mg/mL | 38 mg/mL | -1 mg/mL |
S3821 | Nuciferine | <1 mg/mL | 2 mg/mL | <1 mg/mL |
S8447 | 8-OH-DPAT (8-Hydroxy-DPAT) | <1 mg/mL | 49 mg/mL | 49 mg/mL |
S4256 | Buspirone HCl | 84 mg/mL | 84 mg/mL | 36 mg/mL |
S4639 | Brexpiprazole | <1 mg/mL | 24 mg/mL | '<1 mg/mL |
S4839 | Mosapride | -1 mg/mL | 84 mg/mL | -1 mg/mL |
S4751 | Cisapride hydrate | <1 mg/mL | 96 mg/mL | <1 mg/mL |
S2025 | Urapidil HCl | 85 mg/mL | 24 mg/mL | 1 mg/mL |
S4244 | Serotonin HCl | 42 mg/mL | 42 mg/mL | 2 mg/mL |
S3716 | Flibanserin | <1 mg/mL | 78 mg/mL | 23 mg/mL |
S5843 | Cinitapride Hydrogen Tartrate | 5 mg/mL | 59 mg/mL | <1 mg/mL |
S5506 | Vortioxetine | <1 mg/mL | 34 mg/mL | 28 mg/mL |
S5858 | Vilazodone | <1 mg/mL | 88 mg/mL | '14 mg/mL |
S0222 | Lvguidingan | ˂1 mg/mL | 54 mg/mL | '54 mg/mL |
S3196 | Azacyclonol | 2 mg/mL | 53 mg/mL | 53 mg/mL |
亜型選択性的な製品
5-HT Receptor製品
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S1333 |
Fluoxetine HClFluoxetine HCl (Lilly110140) is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression. |
![]() ![]() The SWIP phenotype in hlh-17(ns204) animals is unaffected by pretreatment with fluoxetine (C). In all panels, n = 30 animals/rep/strain; dark bars = minus inhibitor; and light bars = plus inhibitor. *P< 0.05; **P<0.005; ***P<0.0005. |
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S2464新 |
SevofluraneSevoflurane (Fluoromethyl) is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics. |
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S1441 |
Venlafaxine HClVenlafaxine HCl is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia. |
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S1869 |
Dapoxetine HClDapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation. |
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S1483 |
IloperidoneIloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia. |
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S8021 |
Vortioxetine (Lu AA21004) HBrVortioxetine (Lu AA21004), a multimodal serotonergic agent, is an antagonist of human (h) serotonin (5-HT)3A receptor and h5-HT7 receptor with Ki of 3.7 nM and 19 nM, respectively. Vortioxetine (Lu AA21004) is also a h5-HT1B receptor partial agonist with Ki of 33 nM and h5-HT1A receptor agonist with Ki of 15 nM, and a human 5-HT transporter (SERT) inhibitor with Ki of 1.6 nM. |
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S1336 |
Fluvoxamine maleateFluvoxamine maleate (MK-264) is a selective serotonin (5-HT) reuptake inhibitor (SSRI), used in the treatment of obsessive-compulsive disorder. |
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S4053 |
Sertraline HClSertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM. |
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S3024 |
LamotrigineLamotrigine (BW-430C) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker. |
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S2541 |
Clomipramine HClClomipramine HCl is a hydrochloride salt of clomipramine which is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively. |
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S4113 |
DesvenlafaxineDesvenlafaxine (WY 45233 Succinate) is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively. |
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S4064 |
Escitalopram OxalateEscitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM. |
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S2084 |
Duloxetine HClDuloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD). |
![]() ![]() Summarized results of dose-dependent effect of duloxetine on the following: (1) the capacity of the AA-irritated bladder and (2) PNS-induced increase in bladder capacity. |
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S3140 |
Milnacipran HClMilnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively. |
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S3183 |
Amitriptyline HClAmitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA). |
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S5239 |
Paroxetine mesylateParoxetine Mesylate is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties. |
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S9239 |
IsocorynoxeineIsocorynoxeine (7-Isocorynoxeine), a major alkaloid found in Uncaria rhynchophylla, exhibits wide beneficial effects on the cardiovascular and cardiocerebral vascular systems. Isocorynoxeine suppress 5-HT2A receptor-mediated current response with IC50 of 72.4 μM. |
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S3817 |
Harmine hydrochlorideHarmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs) and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM. |
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S9258 |
(+)-IsocorynolineIsocorynoxeine, a major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM and shows various beneficial effects, including lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage. |
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S5693 |
Levomilnacipran HydrochlorideLevomilnacipran Hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor with antidepressant activity. |
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S1642 |
MethyldopaMethyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg. |
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S9039 |
AlbiflorinAlbiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity. |
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S4749 |
Citalopram HBrCitalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM. |
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S8183 |
PimavanserinPimavanserin (ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease. |
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S5655 |
VenlafaxineVenlafaxine (Wy 45030) is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia. |
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S5485 |
Desipramine HydrochlorideDesipramine hydrochloride (Desmethylimipramine, Norimipramine, EX-4355, G-35020, JB-8181, NSC-114901) is a dibenzazepine-derivative tricyclic antidepressant that acts as a selective norepinephrine reuptake inhibitor. It also shows weak serotonin reuptake inhibitory, α1-blocking, antihistamine, and anticholinergic effects. |
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S4112 |
Desvenlafaxine SuccinateDesvenlafaxine Succinate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively. |
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S2582 |
Trazodone HClTrazodone HCl (AF-1161, KB-831) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders. |
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S5071 |
DuloxetineDuloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake. |
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S4377 |
Imipramine HClImipramine (Melipramine) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination). |
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S9510 |
Protriptyline hydrochlorideProtriptyline Hydrochloride is the hydrochloride salt form of protriptyline. Protriptyline is a tricyclic secondary amine with antidepressant property which acts by inhibition of serotonin and norepinephrine reuptake. |
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S3175 |
Atomoxetine HClAtomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters. |
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S5563 |
Thioridazine hydrochlorideThioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent. |
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S4740 |
Sodium ferulateSodium ferulate (SF, Ferulic acid sodium salt), the sodium salt of ferulic acid, is a drug used in traditional Chinese medicine for treatment of cardiovascular and cerebrovascular diseases and to prevent thrombosis. |
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S2459 |
ClozapineClozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia. |
![]() ![]() Michaelis-Menten plots illustrate the effects of PGD, individual radix paeonia (Pr) and radix glycyrrhiza (Gr) preparations, and the two individual preparations in combination on the formation of N-demethyl-clozapine (A) and clozapine-N-oxide (B) in the human liver microsomes. Serial concentration of clozapine was coincubated in the presence of herbal preparations. The absence of herbal preparations serves as control (CON). |
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S2493 |
OlanzapineOlanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. |
![]() ![]() Punctuates of LC3 proteins in olanzapine-treated T98 and LN229 cells. Cells were incubated with olanzapine (0, 0.1M, 0.2mM) for 48h and then stained with the anti-LC3 antibody. Cells were examined by fluorescence confocal microscopy. Green: FITC-labeled LC3; Blue: DAPI-labeled nucleus. Magnification: x 400
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S2232 |
KetanserinKetanserin (R41468) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug. |
![]() ![]() Immunofluorescence labeling revealed the comparative protein expression level of c-Myc in the mouse (C57BL/6) hippocampus compared with the control group. ***p < 0.001 vs. sham group, ###p < 0.001 vs. CF+SPS+DMSO group, sssp < 0.001 vs. CF+SPS+ ketanserin group. Bar = 100 μm. Data were presented as mean ± SEM through ANOVA. Groups were compared by performing Bonferroni's test. n = 4.
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S1245 |
Latrepirdine 2HClLatrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. |
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S0779新 |
PirenperonePirenperone (R-47456, R-50656), a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg). |
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S2649新 |
SB 200646SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo. |
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S0476新 |
SCH-23390 hydrochlorideSCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride,SCH-23390 HCl) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM. |
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S0313新 |
VolinanserinVolinanserin (Volinanserin Hydrochloride Salt, MDL100907, M 100907, MDL-100,907) is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity. |
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S2644新 |
LerisetronLerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM. |
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S2698 |
RS-127445RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors. |
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S1243 |
AgomelatineAgomelatine (S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. |
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S1283 |
Asenapine maleateAsenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder. |
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S3005 |
Paroxetine HClParoxetine HCl (BRL-29060A, FG-7051) is an antidepressant drug of the SSRI type. |
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S1615 |
RisperidoneRisperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder. |
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S1444 |
Ziprasidone HClZiprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder. |
![]() ![]() a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM.
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S2663 |
WAY-100635 MaleateWAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM. |
![]() ![]() Effects of antagonists on the anti-hyperalgesic effects of sinomenine in CCI rats. * P , 0.05 as compared to vehicle control group (N=8 per group). The 5-HT1A receptor antagonist WAY100635 does not block the antinociceptive effects of 40 mg/kg sinomenine. |
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S2112 |
BlonanserinBlonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia. |
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S2849 |
SB269970 HClSB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors. |
![]() ![]() Cells transfected with 5-HT7A receptor, were incubated with agonist with or without antagonist, or antagonist with 1 μM agonist. Three independent experiments were performed in triplicate. |
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S1345 |
Granisetron HClGranisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting. |
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S2016 |
MirtazapineMirtazapine (Org3770) is an adrenergic and seroton receptor antagonist, used to treat depression. |
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S2894 |
SB742457SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2. |
![]() ![]() The levels of Aβ produced by SK-N-SH cells in response to the indicated HTR6 antagonists at 1μM, 3μM or 10μM for 24hours
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S2677 |
BRL-15572 DihydrochlorideBRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor. |
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S8010 |
PRX-08066 Maleic acidPRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2. |
![]() ![]() The HTR2B antagonist PRX-08066 reduced the viability of UM metastatic cell lines. MTS cell viability assays were performed 72 h post-treatment with PRX-08066. Increasing concentrations of PRX-08066 (5, 10, 20, 50 and 100 µM) were tested on UM metastatic cell lines T111, T128 and T131 (a). The 20 µM concentration was tested on UM non-metastatic cell lines (T108, T130 and T143) and normal uveal melanocytes (NUM; b). Data are represented as relative percentage of viability using a column bar graph (mean±SEM). The absorbance of untreated cells (black bars) was considered as 100%. Student t test, *P<0.05
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S1390 |
Ondansetron HClOndansetron HCl (GR 38032F) is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy. |
![]() ![]() Mean (±SEM) cumulative 5-HT concentration–response curves in the absence and presence of 5-HT antagonists (n = >8). Responses are expressed as a percentage of the maximum response for each curve.
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S1898 |
Tropisetron HClTropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy. |
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S1394 |
Pizotifen MalatePizotifen Malate (BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches. |
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S2106 |
Azasetron HClAzasetron HCl (Y-25130) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. |
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S4249 |
FlopropioneFlopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist. |
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S4086 |
Loxapine SuccinateLoxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent. |
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S1996 |
OndansetronOndansetron (GR 38032F, GR-C507/75) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic. |
![]() ![]() Mean (±SEM) cumulative 5-HT concentration–response curves in the absence and presence of 5-HT antagonists (n = >8). Responses are expressed as a percentage of the maximum response for each curve.
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S2856 |
SB 271046 hydrochlorideSB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes. |
![]() ![]() The levels of Aβ produced by SK-N-SH cells in response to the indicated HTR6 antagonists at 1μM, 3μM or 10μM for 24hours
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S5326 |
DolasetronDolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. It has minimal activity at other known serotonin receptors, and has low affinity for dopamine receptors. |
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S5472 |
Nafronyl oxalate saltNafronyl oxalate salt is the oxalate salt form of nafronyl, which is a selective antagonist of 5-HT2 receptors and a vasodilator used in the management of peripheral and cerebral vascular disorders. |
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S3050 |
Palonosetron HClPalonosetron HCl (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting. |
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S4889 |
Perospirone hydrochloridePerospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist. |
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S5857 |
TrazodoneTrazodone is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders. |
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S3054 |
Alverine CitrateAlverine citrate (NSC 35459) is a drug used for functional gastrointestinal disorders. |
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S2865 |
VUF 10166VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower. |
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S5947 |
AmitriptylineAmitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. |
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S5398 |
Nefazodone hydrochlorideNefazodone hydrochloride (BMY-13754-1) is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake. |
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S4635 |
Cyproheptadine hydrochloride sesquihydrateCyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor. |
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S4748 |
Ondansetron Hydrochloride DihydrateOndansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors. |
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S4694 |
Alosetron HydrochlorideAlosetron Hydrochloride (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. |
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S5714 |
lurasidoneLurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors. |
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S3706 |
Sarpogrelate hydrochlorideSarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively. |
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S3723 |
Ramosetron HydrochlorideRamosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. |
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S2346 |
PuerarinPuerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist. |
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S5538 |
TropisetronTropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
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S5428 |
Promazine hydrochloridePromazine (Romtiazin, Sinophenin) is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors with antipsychotic effects. |
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S4283 |
Cyclobenzaprine HClCyclobenzaprine HCl is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist. |
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S5052 |
GranisetronGranisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy. |
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S5749 |
ChlorpromazineChlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM. |
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S2669 |
LY310762 HClLY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor. |
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S9174 |
XanthotoxolXanthotoxol (8-Hydroxypsoralen, 8-Hydroxypsoralene, 8-Hydroxyfuranocoumarin, Psoralen), a biologically active linear furocoumarin found in a large number of plants, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects. |
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S5740 |
PalonosetronPalonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with pKi value of 10.45. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). |
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S5060 |
MetadoxineMetadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. |
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S0496新 |
PF-04995274PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. |
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S0104新 |
Pardoprunox (SLV-308) hydrochloridePardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively. |
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S2578新 |
1-Phenylbiguanide1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM. |
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S1436 |
Tianeptine sodiumTianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes. |
![]() ![]() Tianeptine is a full agonist at μ-opioid receptors (MORs). The mouse MOR was co-expressed with GαoB, β1, γ2 and the BRET sensor CAMYEL to measure the inhibition of cAMP inhibition by tianeptine and the MOR agonist DAMGO. Naltrexone dose-dependently inhibits cAMP inhibition by both DAMGO and tianeptine with an IC50 of 35.3±2.3 and 23.3±3.9 nM, respectively. Data represent mean±s.e.m. of six independent experiments.
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S1432 |
Sumatriptan SuccinateSumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches. |
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S2875 |
PrucalopridePrucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes. |
![]() ![]() Concentration-dependent facilitation by prucalopride of electrically induced submaximal cholinergic contractions. Influence of 0.003, 0.01 and 0.03 μmol/L prucalopride, administered to separate strips (A-C) and of 0.3 nmol/L to 1 μmol/L prucalopride, added cumulatively (D-F) on submaximal electrically induced cholinergic contractions at V50% (10 seconds trains at 4 Hz [fundus] or 8 Hz [jejunum and colon], 0.5 milliseconds, interval of 5 [fundus and colon] or 10 minutes [jejunum]) in murine fundus (A,D), jejunum (B,E) and colon (C,F). Contractions are expressed as percentage of the mean of the five contractions before adding prucalopride. Experiments were performed in the continuous presence of 4 μmol/L guanethidine, 300 μmol/L l-NAME and for colon also 1 μmol/L MRS 2500. Means±SEM; ns not significant, *P<.05, **P<.01, ***P<.001 vs control (one-way ANOVA with Bonferroni corrected t test) |
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S1975 |
AripiprazoleAripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist. |
![]() ![]() Olanzapine and aripiprazole differentially regulate cellular glucose uptake of PBMC. Bar graphs depict cellular glucose uptake assessed by 18F-FDG in PBMC after 72 h of stimulation with the indicated concentrations of olanzapine (Olan, A) or aripiprazole (Arip, B) relative to corresponding DMSO controls (Ctrl) and normalized to protein content. Data are depicted as mean ± SD. P-values were computed by one-way ANOVA followed by Dunnett's Multiple Comparison Test. ***P < 0.001, **P < 0.01, *P < 0.05 versus control; results were obtained from n = 4e-6 independent cell isolations measured in duplicate
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S1488 |
Naratriptan HClNaratriptan HCl is a triptan agent that is used for the treatment of migraine headaches. |
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S1607 |
Rizatriptan BenzoateRizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks. |
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S1649 |
ZolmitriptanZolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines. |
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S1385 |
Mosapride CitrateMosapride Citrate (AS-4370) is a gastroprokinetic agent that acts as a selective 5HT4 agonist. |
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S3180 |
Eletriptan HBrEletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively. |
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S4247 |
Prucalopride SuccinatePrucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively. |
![]() ![]() Prucalopride in the presence of IBMX on the S2/S1 ratio of electrically induced total tritium outflow. Tissues were stimulated twice (S1 and S2; 1 millisecond, 15 V, 4 Hz, 2 minutes); IBMX was added 36 minutes and prucalopride 15 minutes before S2. Mean S2/S1±SEM; one‐way ANOVA followed by Bonferroni corrected t test with ns not significant, *P<.05 and ***P<.001.
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S4259 |
Vilazodone HClVilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder. |
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S2096 |
Almotriptan MalateAlmotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. |
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S5741 |
QuetiapineQuetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.23, 5.74, 7.54, 5.55. |
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S5848 |
Frovatriptan SuccinateFrovatriptan Succinate is the succinate salt form of frovatriptan, a synthetic triptan with serotonin (5-HT) receptor agonist activity especially for the 5-HT1B/1D receptors. |
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S6489 |
Lasmiditan succinateLasmiditan succinate (COL-144, LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity. |
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S5401 |
Tegaserod MaleateTegaserod Maleate is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors. |
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S2852 |
BRL-54443BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. |
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S5153 |
TetrahydroberberineTetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors. |
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S5253 |
CisaprideCisapride (Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects. |
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S6324 |
5-Methoxytryptamine5-Methoxytryptamine (Mexamine, Methoxytryptamine) is a tryptamine derivative that acts as a full agonist at the 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7 receptors. |
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S3821 |
NuciferineNuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. |
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S8447 |
8-OH-DPAT (8-Hydroxy-DPAT)8-OH-DPAT (8-Hydroxy-DPAT) is a kind of classic 5-HT1A agonist with the pIC50 of 8.19. It has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site; Its biological half-life is 1.5 hous. |
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S4256 |
Buspirone HClBuspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. |
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S4639 |
BrexpiprazoleBrexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. |
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S4839 |
MosaprideMosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. |
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S4751 |
Cisapride hydrateCisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic. |
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S2025 |
Urapidil HClUrapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. |
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S4244 |
Serotonin HClSerotonin HCl (5-HT) is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist. |
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S3716 |
FlibanserinFlibanserin (BIMT-17, BIMT-17-BS) is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors. |
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S5843 |
Cinitapride Hydrogen TartrateCinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors |
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S5506 |
VortioxetineVortioxetine, a novel antidepressant for the treatment of major depressive disorder, is a 5-HT3, 5-HT7 and 5-HT1D receptor antagonist, 5-HT1B receptor partial agonist, 5-HT1A receptor agonist and serotonin (5-HT) transporter (SERT) inhibitor. |
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S5858 |
VilazodoneVilazodone (EMD-68843, SB-659746A) is a novel antidepressant having a selective serotonin (5-HT) reuptake inhibitory and 5-HT1A receptor partial agonist activity. The affinity of vilazodone is much higher in the 5-HT reuptake site (Ki=0.1 nM) than in norepinephrine (Ki=56 nM) and dopamine (Ki=37 nM) sites. |
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S0222新 |
LvguidinganLvguidingan (Anticonvulsant 7903, 3,4-dichlorophenyl propenylisobutylamide) is an anticonvulsant/antiepileptic agent. Lvguidingan (Anticonvulsant 7903) is found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain. |
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S3196 |
AzacyclonolAzacyclonol (MER 17, MDL 4829), also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S1333 |
Fluoxetine HClFluoxetine HCl (Lilly110140) is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression. |
![]() ![]() The SWIP phenotype in hlh-17(ns204) animals is unaffected by pretreatment with fluoxetine (C). In all panels, n = 30 animals/rep/strain; dark bars = minus inhibitor; and light bars = plus inhibitor. *P< 0.05; **P<0.005; ***P<0.0005. |
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S2464新 |
SevofluraneSevoflurane (Fluoromethyl) is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics. |
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S1441 |
Venlafaxine HClVenlafaxine HCl is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia. |
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S1869 |
Dapoxetine HClDapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation. |
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S1483 |
IloperidoneIloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia. |
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S8021 |
Vortioxetine (Lu AA21004) HBrVortioxetine (Lu AA21004), a multimodal serotonergic agent, is an antagonist of human (h) serotonin (5-HT)3A receptor and h5-HT7 receptor with Ki of 3.7 nM and 19 nM, respectively. Vortioxetine (Lu AA21004) is also a h5-HT1B receptor partial agonist with Ki of 33 nM and h5-HT1A receptor agonist with Ki of 15 nM, and a human 5-HT transporter (SERT) inhibitor with Ki of 1.6 nM. |
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S1336 |
Fluvoxamine maleateFluvoxamine maleate (MK-264) is a selective serotonin (5-HT) reuptake inhibitor (SSRI), used in the treatment of obsessive-compulsive disorder. |
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S4053 |
Sertraline HClSertraline HCl (CP-51974-1) is a 5-HT antagonist with Ki of 13 nM. |
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S3024 |
LamotrigineLamotrigine (BW-430C) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker. |
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S2541 |
Clomipramine HClClomipramine HCl is a hydrochloride salt of clomipramine which is a serotonin transporter (SERT), norepinephrine transporter (NET) dopamine transporter (DAT) blocker with Ki of 0.14, 54 and 3 nM, respectively. |
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S4113 |
DesvenlafaxineDesvenlafaxine (WY 45233 Succinate) is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively. |
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S4064 |
Escitalopram OxalateEscitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM. |
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S2084 |
Duloxetine HClDuloxetine HCl (LY-248686) is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD). |
![]() ![]() Summarized results of dose-dependent effect of duloxetine on the following: (1) the capacity of the AA-irritated bladder and (2) PNS-induced increase in bladder capacity. |
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S3140 |
Milnacipran HClMilnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively. |
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S3183 |
Amitriptyline HClAmitriptyline HCl is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline HCl also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. Amitriptyline is a tricyclic antidepressant (TCA). |
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S5239 |
Paroxetine mesylateParoxetine Mesylate is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties. |
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S9239 |
IsocorynoxeineIsocorynoxeine (7-Isocorynoxeine), a major alkaloid found in Uncaria rhynchophylla, exhibits wide beneficial effects on the cardiovascular and cardiocerebral vascular systems. Isocorynoxeine suppress 5-HT2A receptor-mediated current response with IC50 of 72.4 μM. |
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S3817 |
Harmine hydrochlorideHarmine (Telepathine), a fluorescent harmala alkaloid belonging to the beta-carboline family of compounds, is a highly cell-permeant and competitive inhibitor of ATP binding to the kinase pocket of DYRK1A, with about 60-fold higher IC50 value for DYRK2. Harmine also inhibits monoamine oxidases (MAOs) and cdc-like kinases (CLKs). Harmine inhibits 5-HT2A serotonin receptor with Ki of 397 nM. |
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S9258 |
(+)-IsocorynolineIsocorynoxeine, a major bioactive tetracyclic oxindole alkaloids found in Uncaria rhynchophylla, exhibits a dose-dependent inhibition of 5-HT2A receptor-mediated current response with an IC50 of 72.4 μM and shows various beneficial effects, including lowering blood pressure, vasodilatation, and protection against ischemia-induced neuronal damage. |
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S5693 |
Levomilnacipran HydrochlorideLevomilnacipran Hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor with antidepressant activity. |
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S1642 |
MethyldopaMethyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg. |
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S9039 |
AlbiflorinAlbiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity. |
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S4749 |
Citalopram HBrCitalopram HBr (Nitalapram HBr, Prepram HBr, Bonitrile HBr, Lu 10-171 HBr), an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM. |
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S8183 |
PimavanserinPimavanserin (ACP-103) is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease. |
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S5655 |
VenlafaxineVenlafaxine (Wy 45030) is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia. |
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S5485 |
Desipramine HydrochlorideDesipramine hydrochloride (Desmethylimipramine, Norimipramine, EX-4355, G-35020, JB-8181, NSC-114901) is a dibenzazepine-derivative tricyclic antidepressant that acts as a selective norepinephrine reuptake inhibitor. It also shows weak serotonin reuptake inhibitory, α1-blocking, antihistamine, and anticholinergic effects. |
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S4112 |
Desvenlafaxine SuccinateDesvenlafaxine Succinate (WY 45233) is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively. |
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S2582 |
Trazodone HClTrazodone HCl (AF-1161, KB-831) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders. |
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S5071 |
DuloxetineDuloxetine (LY-248686) is a potent inhibitor of serotonin (5-hydroxytryptamine, 5-HT) and noradrenaline (NE) uptake in vitro and in vivo and is 3- to 5-times more effective at inhibiting 5-HT uptake. |
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S4377 |
Imipramine HClImipramine (Melipramine) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination). |
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S9510 |
Protriptyline hydrochlorideProtriptyline Hydrochloride is the hydrochloride salt form of protriptyline. Protriptyline is a tricyclic secondary amine with antidepressant property which acts by inhibition of serotonin and norepinephrine reuptake. |
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S3175 |
Atomoxetine HClAtomoxetine (LY 139603) is a selective norepinephrine (NE) transporter inhibitor with Ki of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters. |
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S5563 |
Thioridazine hydrochlorideThioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S4740 |
Sodium ferulateSodium ferulate (SF, Ferulic acid sodium salt), the sodium salt of ferulic acid, is a drug used in traditional Chinese medicine for treatment of cardiovascular and cerebrovascular diseases and to prevent thrombosis. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S2459 |
ClozapineClozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia. |
2020, 10.1002/ana.25935 2018, 18(1):89 2016, 21(6) |
![]() ![]() Michaelis-Menten plots illustrate the effects of PGD, individual radix paeonia (Pr) and radix glycyrrhiza (Gr) preparations, and the two individual preparations in combination on the formation of N-demethyl-clozapine (A) and clozapine-N-oxide (B) in the human liver microsomes. Serial concentration of clozapine was coincubated in the presence of herbal preparations. The absence of herbal preparations serves as control (CON). |
S2493 |
OlanzapineOlanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. |
2020, S0092-8674(20)31394-5 2020, 10.1038/s41401-020-0378-6 2019, 560:294-305 |
![]() ![]() Punctuates of LC3 proteins in olanzapine-treated T98 and LN229 cells. Cells were incubated with olanzapine (0, 0.1M, 0.2mM) for 48h and then stained with the anti-LC3 antibody. Cells were examined by fluorescence confocal microscopy. Green: FITC-labeled LC3; Blue: DAPI-labeled nucleus. Magnification: x 400
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S2232 |
KetanserinKetanserin (R41468) is a specific 5-HT2A serotonin receptor antagonist with Ki of 2.5 nM for rat and human 5-HT2A, used as an antihypertensive drug. |
2019, 10.1016/j.intimp.2019.106036 2018, 8(1):15753 2017, 25(1):39-53 |
![]() ![]() Immunofluorescence labeling revealed the comparative protein expression level of c-Myc in the mouse (C57BL/6) hippocampus compared with the control group. ***p < 0.001 vs. sham group, ###p < 0.001 vs. CF+SPS+DMSO group, sssp < 0.001 vs. CF+SPS+ ketanserin group. Bar = 100 μm. Data were presented as mean ± SEM through ANOVA. Groups were compared by performing Bonferroni's test. n = 4.
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S1245 |
Latrepirdine 2HClLatrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug. |
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S0779新 |
PirenperonePirenperone (R-47456, R-50656), a quinazoline derivative, is a selective antagonist of SR-2A (5-HT2 serotonin receptor) when employed in low doses. Pirenperone behaves like a typical neuroleptic when used in higher doses (greater than 0.1 mg/kg). |
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S2649新 |
SB 200646SB 200646 (SB 200646A) is a potent, selective and oral-active antagonist of 5-HT2B/2C over 5-HT2A receptor with 50 fold selectivity. The pKi for rat 5-HT2C receptor, rat 5-HT2B receptor and rat 5-HT2A receptor are 6.9, 7.5 and 5.2, respectively. SB 200646 has electrophysiological and anxiolytic properties in vivo. |
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S0476新 |
SCH-23390 hydrochlorideSCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride,SCH-23390 HCl) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM. |
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S0313新 |
VolinanserinVolinanserin (Volinanserin Hydrochloride Salt, MDL100907, M 100907, MDL-100,907) is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity. |
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S2644新 |
LerisetronLerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM. |
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S2698 |
RS-127445RS-127445 (MT500) is a selective 5-HT2B receptor antagonist with pKi of 9.5 and pIC50 of 10.4, exhibits >1000-fold selectivity against other 5-HT receptors. |
2019, 10.1016/j.intimp.2019.106036 2018, 9:587 |
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S1243 |
AgomelatineAgomelatine (S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor. |
2018, 8(1):15753 2017, 82:11-18 |
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S1283 |
Asenapine maleateAsenapine maleate (Org 5222) is a high-affinity antagonist of serotonin, norepinephrine, dopamine and histamine receptors, used for the treatment of schizophrenia and acute mania associated with bipolar disorder. |
2018, 8(1):15753 |
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S3005 |
Paroxetine HClParoxetine HCl (BRL-29060A, FG-7051) is an antidepressant drug of the SSRI type. |
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S1615 |
RisperidoneRisperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder. |
2018, 18(1):89 |
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S1444 |
Ziprasidone HClZiprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder. |
2018, 560(7718):372-376 2018, 8(1):15753 2017, 7(1):8491 |
![]() ![]() a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM.
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S2663 |
WAY-100635 MaleateWAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM. |
2019, 20(1):16.e1-16.e16 2018, 43(7):1371-1382 2017, 12(1):e0168964 |
![]() ![]() Effects of antagonists on the anti-hyperalgesic effects of sinomenine in CCI rats. * P , 0.05 as compared to vehicle control group (N=8 per group). The 5-HT1A receptor antagonist WAY100635 does not block the antinociceptive effects of 40 mg/kg sinomenine. |
S2112 |
BlonanserinBlonanserin (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia. |
2018, 8(1):15753 |
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S2849 |
SB269970 HClSB269970 HCl is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3, exhibits >50-fold selectivity against other receptors. |
2018, 10.1089/neu.2018.5652 2015, 5:8060 |
![]() ![]() Cells transfected with 5-HT7A receptor, were incubated with agonist with or without antagonist, or antagonist with 1 μM agonist. Three independent experiments were performed in triplicate. |
S1345 |
Granisetron HClGranisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting. |
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S2016 |
MirtazapineMirtazapine (Org3770) is an adrenergic and seroton receptor antagonist, used to treat depression. |
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S2894 |
SB742457SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2. |
2018, 8(1):15753 2017, 7(1):4983 |
![]() ![]() The levels of Aβ produced by SK-N-SH cells in response to the indicated HTR6 antagonists at 1μM, 3μM or 10μM for 24hours
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S2677 |
BRL-15572 DihydrochlorideBRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor. |
2018, 74:49-67 2018, 10.1213/ANE.0000000000003757 2018, 56:168-178 |
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S8010 |
PRX-08066 Maleic acidPRX-08066 Maleic acid is a selective 5-HT2B receptor antagonist with IC50 of 3.4 nM, prevents the severity of pulmonary arterial hypertension in the MCT rat model. Phase 2. |
2018, 35(3):123-134 |
![]() ![]() The HTR2B antagonist PRX-08066 reduced the viability of UM metastatic cell lines. MTS cell viability assays were performed 72 h post-treatment with PRX-08066. Increasing concentrations of PRX-08066 (5, 10, 20, 50 and 100 µM) were tested on UM metastatic cell lines T111, T128 and T131 (a). The 20 µM concentration was tested on UM non-metastatic cell lines (T108, T130 and T143) and normal uveal melanocytes (NUM; b). Data are represented as relative percentage of viability using a column bar graph (mean±SEM). The absorbance of untreated cells (black bars) was considered as 100%. Student t test, *P<0.05
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S1390 |
Ondansetron HClOndansetron HCl (GR 38032F) is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy. |
2019, 50(5):1163-1171 2016, 23(11):946-951 |
![]() ![]() Mean (±SEM) cumulative 5-HT concentration–response curves in the absence and presence of 5-HT antagonists (n = >8). Responses are expressed as a percentage of the maximum response for each curve.
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S1898 |
Tropisetron HClTropisetron HCl (ICS 205-930) is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy. |
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S1394 |
Pizotifen MalatePizotifen Malate (BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches. |
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S2106 |
Azasetron HClAzasetron HCl (Y-25130) is a selective 5-HT3 receptor antagonist with IC50 of 0.33 nM used in the management of nausea and vomiting induced by cancer chemotherapy. |
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S4249 |
FlopropioneFlopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist. |
2020, 10:2936 |
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S4086 |
Loxapine SuccinateLoxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent. |
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S1996 |
OndansetronOndansetron (GR 38032F, GR-C507/75) is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic. |
2016, 23(11):946-951 |
![]() ![]() Mean (±SEM) cumulative 5-HT concentration–response curves in the absence and presence of 5-HT antagonists (n = >8). Responses are expressed as a percentage of the maximum response for each curve.
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S2856 |
SB 271046 hydrochlorideSB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9, exhibits 200-fold greater selectivity over other 5-HT receptor subtypes. |
2018, 8(1):15753 |
![]() ![]() The levels of Aβ produced by SK-N-SH cells in response to the indicated HTR6 antagonists at 1μM, 3μM or 10μM for 24hours
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S5326 |
DolasetronDolasetron is a highly specific and selective serotonin 5-HT3 receptor antagonist. It has minimal activity at other known serotonin receptors, and has low affinity for dopamine receptors. |
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S5472 |
Nafronyl oxalate saltNafronyl oxalate salt is the oxalate salt form of nafronyl, which is a selective antagonist of 5-HT2 receptors and a vasodilator used in the management of peripheral and cerebral vascular disorders. |
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S3050 |
Palonosetron HClPalonosetron HCl (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting. |
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S4889 |
Perospirone hydrochloridePerospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist. |
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S5857 |
TrazodoneTrazodone is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders. |
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S3054 |
Alverine CitrateAlverine citrate (NSC 35459) is a drug used for functional gastrointestinal disorders. |
2018, 315(2):L133-L148 |
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S2865 |
VUF 10166VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with Ki of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower. |
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S5947 |
AmitriptylineAmitriptyline (MK-230, N-750, Ro41575) is a tricyclic antidepressant (TCA) with analgesic properties, widely used to treat depression and neuropathic pain. Amitriptyline is an inhibitor of both serotonin transporter (SERT) and norepinephrine transporter (NET) with Ki of 3.45 nM and 13.3 nM, respectively. Amitriptyline also inhibits histamine receptor H1, histamine receptor H4, 5-HT2 and sigma 1 receptor with Ki of 0.5 nM, 7.31 nM, 235 nM and 287 nM, respectively. |
2019, 11(12) |
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S5398 |
Nefazodone hydrochlorideNefazodone hydrochloride (BMY-13754-1) is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake. |
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S4635 |
Cyproheptadine hydrochloride sesquihydrateCyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor. |
2019, 39(7):3767-3775 |
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S4748 |
Ondansetron Hydrochloride DihydrateOndansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors. |
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S4694 |
Alosetron HydrochlorideAlosetron Hydrochloride (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist. |
2017, 170(1):185-198 |
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S5714 |
lurasidoneLurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. It also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors. |
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S3706 |
Sarpogrelate hydrochlorideSarpogrelate (MCI-9042) is a selective 5-HT2A antagonist with pKi values of 8.52, 7.43 and 6.57 for 5-HT2A, 5-HT2C and 5-HT2B receptors respectively. |
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S3723 |
Ramosetron HydrochlorideRamosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity. |
2020, 10(16):7351-7368 |
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S2346 |
PuerarinPuerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist. |
2020, 21(14):5025 2019, 73(6):373-382 2019, 91(8):1440-1447 |
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S5538 |
TropisetronTropisetron (ICS 205-930) is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor. |
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S5428 |
Promazine hydrochloridePromazine (Romtiazin, Sinophenin) is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors with antipsychotic effects. |
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S4283 |
Cyclobenzaprine HClCyclobenzaprine HCl is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist. |
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S5052 |
GranisetronGranisetron (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy. |
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S5749 |
ChlorpromazineChlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM. |
2020, 232:119701 2020, 48(8):613-621 2020, 2020/9/20.4.7.30734 |
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S2669 |
LY310762 HClLY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor. |
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S9174 |
XanthotoxolXanthotoxol (8-Hydroxypsoralen, 8-Hydroxypsoralene, 8-Hydroxyfuranocoumarin, Psoralen), a biologically active linear furocoumarin found in a large number of plants, shows strong pharmacological activities as anti-inflammatory, antioxidant, 5-HT antagonistic, and neuroprotective effects. |
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S5740 |
PalonosetronPalonosetron (RS25259, RS 25259 197) is a 5-HT3 antagonist with pKi value of 10.45. It is used in the prevention and treatment of chemotherapy-induced nausea and vomiting (CINV). |
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S5060 |
MetadoxineMetadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S0496新 |
PF-04995274PF-04995274 (PF-4995274) is a potent, high-affinity, orally active and partial agonist of serotonin 4 receptor (5-HT4R) with EC50 of 0.47 nM, 0.36 nM, 0.37 nM and 0.26 nM for human 5-HT4A/4B/4D/4E, respectively. As for rat 5-HT4S/4L/4E, the EC50 is 0.59 nM, 0.65 nM and 0.62 nM, respectively. PF-04995274 is brain penetrant and can be used for cognitive disorders associated with Alzheimer's disease. |
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S0104新 |
Pardoprunox (SLV-308) hydrochloridePardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively. |
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S2578新 |
1-Phenylbiguanide1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM. |
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S1436 |
Tianeptine sodiumTianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes. |
2014, 4:e411 |
![]() ![]() Tianeptine is a full agonist at μ-opioid receptors (MORs). The mouse MOR was co-expressed with GαoB, β1, γ2 and the BRET sensor CAMYEL to measure the inhibition of cAMP inhibition by tianeptine and the MOR agonist DAMGO. Naltrexone dose-dependently inhibits cAMP inhibition by both DAMGO and tianeptine with an IC50 of 35.3±2.3 and 23.3±3.9 nM, respectively. Data represent mean±s.e.m. of six independent experiments.
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S1432 |
Sumatriptan SuccinateSumatriptan Succinate (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches. |
2017, 42(6):755-761 |
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S2875 |
PrucalopridePrucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes. |
2019, 68(8):1406-1416 2017, 9(12) 2017, 10.1111/nmo.13064 |
![]() ![]() Concentration-dependent facilitation by prucalopride of electrically induced submaximal cholinergic contractions. Influence of 0.003, 0.01 and 0.03 μmol/L prucalopride, administered to separate strips (A-C) and of 0.3 nmol/L to 1 μmol/L prucalopride, added cumulatively (D-F) on submaximal electrically induced cholinergic contractions at V50% (10 seconds trains at 4 Hz [fundus] or 8 Hz [jejunum and colon], 0.5 milliseconds, interval of 5 [fundus and colon] or 10 minutes [jejunum]) in murine fundus (A,D), jejunum (B,E) and colon (C,F). Contractions are expressed as percentage of the mean of the five contractions before adding prucalopride. Experiments were performed in the continuous presence of 4 μmol/L guanethidine, 300 μmol/L l-NAME and for colon also 1 μmol/L MRS 2500. Means±SEM; ns not significant, *P<.05, **P<.01, ***P<.001 vs control (one-way ANOVA with Bonferroni corrected t test) |
S1975 |
AripiprazoleAripiprazole (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist. |
2018, 18(1):89 2018, 105:95-102 2018, 38(9):5101-5108 |
![]() ![]() Olanzapine and aripiprazole differentially regulate cellular glucose uptake of PBMC. Bar graphs depict cellular glucose uptake assessed by 18F-FDG in PBMC after 72 h of stimulation with the indicated concentrations of olanzapine (Olan, A) or aripiprazole (Arip, B) relative to corresponding DMSO controls (Ctrl) and normalized to protein content. Data are depicted as mean ± SD. P-values were computed by one-way ANOVA followed by Dunnett's Multiple Comparison Test. ***P < 0.001, **P < 0.01, *P < 0.05 versus control; results were obtained from n = 4e-6 independent cell isolations measured in duplicate
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S1488 |
Naratriptan HClNaratriptan HCl is a triptan agent that is used for the treatment of migraine headaches. |
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S1607 |
Rizatriptan BenzoateRizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks. |
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S1649 |
ZolmitriptanZolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines. |
2019, 560:294-305 |
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S1385 |
Mosapride CitrateMosapride Citrate (AS-4370) is a gastroprokinetic agent that acts as a selective 5HT4 agonist. |
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S3180 |
Eletriptan HBrEletriptan (UK-116044) is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively. |
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S4247 |
Prucalopride SuccinatePrucalopride is a selective, high affinity 5-HT4 receptor agonist. The Ki values of prucalopride for human 5-HT(4a) and 5-HT(4b) receptor are 2.5 nM and 8 nM, respectively. |
2018, 9:171 2018, 30(2) 2017, 29(8) |
![]() ![]() Prucalopride in the presence of IBMX on the S2/S1 ratio of electrically induced total tritium outflow. Tissues were stimulated twice (S1 and S2; 1 millisecond, 15 V, 4 Hz, 2 minutes); IBMX was added 36 minutes and prucalopride 15 minutes before S2. Mean S2/S1±SEM; one‐way ANOVA followed by Bonferroni corrected t test with ns not significant, *P<.05 and ***P<.001.
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S4259 |
Vilazodone HClVilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder. |
2017, 74(3):765-775 |
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S2096 |
Almotriptan MalateAlmotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults. |
2017, 9(3):3507-3518 2016, 7(9):9975-92 |
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S5741 |
QuetiapineQuetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.23, 5.74, 7.54, 5.55. |
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S5848 |
Frovatriptan SuccinateFrovatriptan Succinate is the succinate salt form of frovatriptan, a synthetic triptan with serotonin (5-HT) receptor agonist activity especially for the 5-HT1B/1D receptors. |
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S6489 |
Lasmiditan succinateLasmiditan succinate (COL-144, LY573144) is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity. |
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S5401 |
Tegaserod MaleateTegaserod Maleate is a hydrogen maleate salt form of tegaserod, which is a 5-HT4 receptor partial agonist and binds with high affinity to 5-HT4 receptors. It has limited affinity for 5-HT1 receptors and no appreciable affinity for other 5-HT receptors, muscarinic, adrenergic, dopaminergic or opiate receptors. |
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S2852 |
BRL-54443BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors. |
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S5153 |
TetrahydroberberineTetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors. |
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S5253 |
CisaprideCisapride (Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects. |
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S6324 |
5-Methoxytryptamine5-Methoxytryptamine (Mexamine, Methoxytryptamine) is a tryptamine derivative that acts as a full agonist at the 5-HT1, 5-HT2, 5-HT4, 5-HT6, and 5-HT7 receptors. |
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S3821 |
NuciferineNuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. |
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S8447 |
8-OH-DPAT (8-Hydroxy-DPAT)8-OH-DPAT (8-Hydroxy-DPAT) is a kind of classic 5-HT1A agonist with the pIC50 of 8.19. It has a selectivity of almost-1000 fold for a subtype of the 5-HT1 binding site; Its biological half-life is 1.5 hous. |
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S4256 |
Buspirone HClBuspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. |
2020, 30;141:111394 |
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S4639 |
BrexpiprazoleBrexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors. |
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S4839 |
MosaprideMosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist. |
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S4751 |
Cisapride hydrateCisapride (Propulsid, Alimix, Propulsin, Enteropride, Kinestase) acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic. |
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S2025 |
Urapidil HClUrapidil HCl is a hydrochloride salt form of urapidil which is α1-adrenoceptor antagonist and 5-HT1A receptor agonist with pIC50 of 6.13 and 6.4 respectively. |
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S4244 |
Serotonin HClSerotonin HCl (5-HT) is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S3716 |
FlibanserinFlibanserin (BIMT-17, BIMT-17-BS) is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors. |
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S5843 |
Cinitapride Hydrogen TartrateCinitapride Hydrogen Tartrate is a gastroprokinetic agent that acts as an agonist of the 5-HT1 and 5-HT4 receptors and as an antagonist of the 5-HT2 receptors |
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S5506 |
VortioxetineVortioxetine, a novel antidepressant for the treatment of major depressive disorder, is a 5-HT3, 5-HT7 and 5-HT1D receptor antagonist, 5-HT1B receptor partial agonist, 5-HT1A receptor agonist and serotonin (5-HT) transporter (SERT) inhibitor. |
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S5858 |
VilazodoneVilazodone (EMD-68843, SB-659746A) is a novel antidepressant having a selective serotonin (5-HT) reuptake inhibitory and 5-HT1A receptor partial agonist activity. The affinity of vilazodone is much higher in the 5-HT reuptake site (Ki=0.1 nM) than in norepinephrine (Ki=56 nM) and dopamine (Ki=37 nM) sites. |
製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
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S0222新 |
LvguidinganLvguidingan (Anticonvulsant 7903, 3,4-dichlorophenyl propenylisobutylamide) is an anticonvulsant/antiepileptic agent. Lvguidingan (Anticonvulsant 7903) is found to be able to increase the concentration of 5-HT and 5-HIAA in mice brain. |
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S3196 |
AzacyclonolAzacyclonol (MER 17, MDL 4829), also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals. |
2020, 44(6):2503-2516 |