5-HT受容体

シグナル伝達経路

研究分野

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)
DMSO アルコール
S1333 Fluoxetine HCl 4 mg/mL 69 mg/mL 69 mg/mL
S2464 Sevoflurane ' mg/mL
S4377 Imipramine HCl 63 mg/mL 63 mg/mL 63 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
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
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
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
S5947 Amitriptyline ' mg/mL
S5398 Nefazodone hydrochloride -1 mg/mL 22 mg/mL -1 mg/mL
S4635 Cyproheptadine hydrochloride <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
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
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
S1333

Fluoxetine HCl

Fluoxetine is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.

S2464

Sevoflurane

Sevoflurane is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics.

S4377

Imipramine HCl

Imipramine is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).

S1441

Venlafaxine HCl

Venlafaxine 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.

S1869

Dapoxetine HCl

Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.

S1483

Iloperidone

Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.

S8021

Vortioxetine (Lu AA21004) HBr

Vortioxetine (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.

S1336

Fluvoxamine maleate

Fluvoxamine Maleate is a selective serotonin (5-HT) reuptake inhibitor (SSRI), used in the treatment of obsessive-compulsive disorder.

S4053

Sertraline HCl

Sertraline HCl is a 5-HT antagonist with Ki of 13 nM.

S3024

Lamotrigine

Lamotrigine 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.

S2541

Clomipramine HCl

Clomipramine 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.

S4113

Desvenlafaxine

Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.

S4064

Escitalopram Oxalate

Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.

S2084

Duloxetine HCl

Duloxetine HCl is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).

S3140

Milnacipran HCl

Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively.

S3183

Amitriptyline HCl

Amitriptyline 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).

S5239

Paroxetine mesylate

Paroxetine Mesylate is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties.

S9239

Isocorynoxeine

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.

S9258

(+)-Isocorynoline

Isocorynoxeine, 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.

S5693

Levomilnacipran Hydrochloride

Levomilnacipran Hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor with antidepressant activity.

S1642

Methyldopa

Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.

S9039

Albiflorin

Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity.

S4749

Citalopram HBr

Citalopram HBr, an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.

S8183

Pimavanserin

Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease.

S5655

Venlafaxine

Venlafaxine is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.

S5485

Desipramine Hydrochloride

Desipramine hydrochloride 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.

S4112

Desvenlafaxine Succinate

Desvenlafaxine Succinate is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.

S2582

Trazodone HCl

Trazodone HCl is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.

S5071

Duloxetine

Duloxetine(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.

S9510

Protriptyline hydrochloride

Protriptyline 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.

S3175

Atomoxetine HCl

Atomoxetine 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.

S5563

Thioridazine hydrochloride

Thioridazine is a potent antianxiety and antipsychotic agent.

S4740

Sodium ferulate

Sodium ferulate (SF), 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.

S2459

Clozapine

Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.

S2493

Olanzapine

Olanzapine is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

S2232

Ketanserin

Ketanserin 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.

S1245

Latrepirdine 2HCl

Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.

S0779

Pirenperone

Pirenperone, 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).

S2649

SB 200646

SB 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.

S0313

Volinanserin

Volinanserin is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity.

S2644

Lerisetron

Lerisetron is a 5-HT3 receptor antagonist with IC50 of 0.81μM.

S2698

RS-127445

RS-127445 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.

S1243

Agomelatine

Agomelatine is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.

S1283

Asenapine maleate

Asenapine maleate 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.

S3005

Paroxetine HCl

Paroxetine HCl is an antidepressant drug of the SSRI type.

S1615

Risperidone

Risperidone is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.

S1444

Ziprasidone HCl

Ziprasidone HCl is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.

S2663

WAY-100635 Maleate

WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.

S2112

Blonanserin

Blonanserin is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.

S2849

SB269970 HCl

SB269970 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.

S1345

Granisetron HCl

Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.

S2016

Mirtazapine

Mirtazapine is an adrenergic and seroton receptor antagonist, used to treat depression.

S2894

SB742457

SB742457 is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.

S2677

BRL-15572 Dihydrochloride

BRL-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.

S8010

PRX-08066 Maleic acid

PRX-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.

S1390

Ondansetron HCl

Ondansetron is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.

S1898

Tropisetron HCl

Tropisetron HCl is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

S1394

Pizotifen Malate

Pizotifen Malate is a benzocycloheptane based agent used for recurrent migraine headaches.

S2106

Azasetron HCl

Azasetron HCl 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.

S4249

Flopropione

Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.

S4086

Loxapine Succinate

Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

S1996

Ondansetron

Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.

S2856

SB 271046 hydrochloride

SB 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.

S5326

Dolasetron

Dolasetron 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.

S5472

Nafronyl oxalate salt

Nafronyl 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.

S3050

Palonosetron HCl

Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.

S4889

Perospirone hydrochloride

Perospirone 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.

S5857

Trazodone

Trazodone is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders.

S3054

Alverine Citrate

Alverine citrate is a drug used for functional gastrointestinal disorders.

S2865

VUF 10166

VUF10166 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.

S5947

Amitriptyline

Amitriptyline 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.

S5398

Nefazodone hydrochloride

Nefazodone hydrochloride is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake.

S4635

Cyproheptadine hydrochloride

Cyproheptadine hydrochloride is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.

S4748

Ondansetron Hydrochloride Dihydrate

Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.

S4694

Alosetron Hydrochloride

Alosetron Hydrochloride is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.

S5714

lurasidone

Lurasidone 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.

S3706

Sarpogrelate hydrochloride

Sarpogrelate 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.

S3723

Ramosetron Hydrochloride

Ramosetron Hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.

S2346

Puerarin

Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.

S5538

Tropisetron

Tropisetron is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

S5428

Promazine hydrochloride

Promazine 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.

S4283

Cyclobenzaprine HCl

Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist.

S5052

Granisetron

Granisetron is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.

S2669

LY310762 HCl

LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.

S9174

Xanthotoxol

Xanthotoxol, 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.

S5740

Palonosetron

Palonosetron 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).

S5060

Metadoxine

Metadoxine, also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication.

S2578

1-Phenylbiguanide

1-phenylbiguanide (PBG) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.

S1436

Tianeptine sodium

Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.

S1432

Sumatriptan Succinate

Sumatriptan Succinate is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.

S2875

Prucalopride

Prucalopride 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.

S1975

Aripiprazole

Aripiprazole is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.

S1488

Naratriptan HCl

Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches.

S1607

Rizatriptan Benzoate

Rizatriptan Benzoate is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.

S1649

Zolmitriptan

Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.

S1385

Mosapride Citrate

Mosapride Citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

S3180

Eletriptan HBr

Eletriptan is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.

S4247

Prucalopride Succinate

Prucalopride 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.

S4259

Vilazodone HCl

Vilazodone HCl is a selective serotonin reuptake inhibitor (SSRI) and a partial agonist of 5-HT1A receptors, used for the treatment of major depressive disorder.

S2096

Almotriptan Malate

Almotriptan Malate is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.

S5741

Quetiapine

Quetiapine 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.

S5848

Frovatriptan Succinate

Frovatriptan 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.

S6489

Lasmiditan succinate

Lasmiditan succinate is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity.

S5401

Tegaserod Maleate

Tegaserod 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.

S2852

BRL-54443

BRL 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.

S5153

Tetrahydroberberine

Tetrahydroberberine 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.

S5253

Cisapride

Cisapride is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.

S6324

5-Methoxytryptamine

5-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.

S3821

Nuciferine

Nuciferine 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.

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.

S4256

Buspirone HCl

Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.

S4639

Brexpiprazole

Brexpiprazole 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.

S4839

Mosapride

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

S4751

Cisapride hydrate

Cisapride acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

S2025

Urapidil HCl

Urapidil 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.

S4244

Serotonin HCl

Serotonin HCl is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.

S3716

Flibanserin

Flibanserin is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.

S5843

Cinitapride Hydrogen Tartrate

Cinitapride 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

S5506

Vortioxetine

Vortioxetine, 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.

S5858

Vilazodone

Vilazodone 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.

S0222

Lvguidingan

Lvguidingan (Anticonvulsant 7903) 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.

S3196

Azacyclonol

Azacyclonol, 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
S1333

Fluoxetine HCl

Fluoxetine is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.

S2464

Sevoflurane

Sevoflurane is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics.

S4377

Imipramine HCl

Imipramine is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).

S1441

Venlafaxine HCl

Venlafaxine 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.

S1869

Dapoxetine HCl

Dapoxetine HCl is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.

S1483

Iloperidone

Iloperidone is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.

S8021

Vortioxetine (Lu AA21004) HBr

Vortioxetine (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.

S1336

Fluvoxamine maleate

Fluvoxamine Maleate is a selective serotonin (5-HT) reuptake inhibitor (SSRI), used in the treatment of obsessive-compulsive disorder.

S4053

Sertraline HCl

Sertraline HCl is a 5-HT antagonist with Ki of 13 nM.

S3024

Lamotrigine

Lamotrigine 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.

S2541

Clomipramine HCl

Clomipramine 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.

S4113

Desvenlafaxine

Desvenlafaxine is a serotonin (5-HT) and norepinephrine (NE) reuptake inhibitor with Ki of 40.2 nM and 558.4 nM, respectively.

S4064

Escitalopram Oxalate

Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with Ki of 0.89 nM.

S2084

Duloxetine HCl

Duloxetine HCl is a serotonin-norepinephrine reuptake inhibitor with Ki of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).

S3140

Milnacipran HCl

Milnacipran inhibits both norepinephrine transporter (NET) and norepinephrine transporter (SERT) with IC50 of 77 nM and 420 nM, respectively.

S3183

Amitriptyline HCl

Amitriptyline 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).

S5239

Paroxetine mesylate

Paroxetine Mesylate is the mesylate salt form of paroxetine, a phenylpiperidine derivative and a selective serotonin reuptake inhibitor (SSRI) with antidepressant and anxiolytic properties.

S9239

Isocorynoxeine

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.

S9258

(+)-Isocorynoline

Isocorynoxeine, 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.

S5693

Levomilnacipran Hydrochloride

Levomilnacipran Hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor with antidepressant activity.

S1642

Methyldopa

Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.

S9039

Albiflorin

Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity.

S4749

Citalopram HBr

Citalopram HBr, an antidepressant, is an orally administered selective serotonin reuptake inhibitor (SSRI) with IC50 of 1.8 nM.

S8183

Pimavanserin

Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson’s disease.

S5655

Venlafaxine

Venlafaxine is an arylalkanolamine serotonin-norepinephrine reuptake inhibitor (SNRI), used to treat major depressive disorder (MDD), generalised anxiety disorder (GAD), panic disorder and social phobia.

S5485

Desipramine Hydrochloride

Desipramine hydrochloride 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.

S4112

Desvenlafaxine Succinate

Desvenlafaxine Succinate is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with Ki of 40.2 nM and 558.4 nM respectively.

S2582

Trazodone HCl

Trazodone HCl is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.

S5071

Duloxetine

Duloxetine(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.

S9510

Protriptyline hydrochloride

Protriptyline 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.

S3175

Atomoxetine HCl

Atomoxetine 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.

S5563

Thioridazine hydrochloride

Thioridazine is a potent antianxiety and antipsychotic agent.

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S4740

Sodium ferulate

Sodium ferulate (SF), 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
S2459

Clozapine

Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.

2018, 18(1):89

2016, 21(6)

2015, 43(7):1147-53

S2493

Olanzapine

Olanzapine is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.

2020, 10.1038/s41401-020-0378-6

2019, 560:294-305

2019, 10.1111/cns.13127

S2232

Ketanserin

Ketanserin 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

S1245

Latrepirdine 2HCl

Latrepirdine is an orally active,and neuroactive antagonist of multiple drug targets, including histamine receptors, GluR, and 5-HT receptors, used as an antihistamine drug.

S0779

Pirenperone

Pirenperone, 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).

S2649

SB 200646

SB 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.

S0313

Volinanserin

Volinanserin is a highly selective and potent 5-HT2 receptor antagonist with Ki of 0.36 nM. Volinanserin shows antipsychotic activity.

S2644

Lerisetron

Lerisetron is a 5-HT3 receptor antagonist with IC50 of 0.81μM.

S2698

RS-127445

RS-127445 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

S1243

Agomelatine

Agomelatine 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

S1283

Asenapine maleate

Asenapine maleate 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

S3005

Paroxetine HCl

Paroxetine HCl is an antidepressant drug of the SSRI type.

S1615

Risperidone

Risperidone is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.

2018, 18(1):89

S1444

Ziprasidone HCl

Ziprasidone HCl 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

S2663

WAY-100635 Maleate

WAY-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

S2112

Blonanserin

Blonanserin is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.

2018, 8(1):15753

S2849

SB269970 HCl

SB269970 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

S1345

Granisetron HCl

Granisetron is a serotonin 5-HT3 receptor antagonist,used to treat chemotherapy-induced nausea and vomiting.

S2016

Mirtazapine

Mirtazapine is an adrenergic and seroton receptor antagonist, used to treat depression.

S2894

SB742457

SB742457 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

S2677

BRL-15572 Dihydrochloride

BRL-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

S8010

PRX-08066 Maleic acid

PRX-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

S1390

Ondansetron HCl

Ondansetron 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

S1898

Tropisetron HCl

Tropisetron HCl is a potent and selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist, used to treat nausea and vomiting following chemotherapy.

S1394

Pizotifen Malate

Pizotifen Malate is a benzocycloheptane based agent used for recurrent migraine headaches.

S2106

Azasetron HCl

Azasetron HCl 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.

S4249

Flopropione

Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.

2020, 10:2936

S4086

Loxapine Succinate

Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.

S1996

Ondansetron

Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic.

2016, 23(11):946-951

S2856

SB 271046 hydrochloride

SB 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

S5326

Dolasetron

Dolasetron 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.

S5472

Nafronyl oxalate salt

Nafronyl 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.

S3050

Palonosetron HCl

Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.

S4889

Perospirone hydrochloride

Perospirone 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.

S5857

Trazodone

Trazodone is a 5-HT 2A/2C receptor antagonist that is used as an antidepressant for treating major depressive disorder and anxiety disorders.

S3054

Alverine Citrate

Alverine citrate is a drug used for functional gastrointestinal disorders.

2018, 315(2):L133-L148

S2865

VUF 10166

VUF10166 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.

S5947

Amitriptyline

Amitriptyline 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)

S5398

Nefazodone hydrochloride

Nefazodone hydrochloride is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake.

S4635

Cyproheptadine hydrochloride

Cyproheptadine hydrochloride is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.

2019, 39(7):3767-3775

S4748

Ondansetron Hydrochloride Dihydrate

Ondansetron is a highly specific and selective serotonin 5-HT3 receptor antagonist (Ki=6.16 nM), with low affinity for dopamine receptors.

S4694

Alosetron Hydrochloride

Alosetron Hydrochloride is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.

2017, 170(1):185-198

S5714

lurasidone

Lurasidone 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.

S3706

Sarpogrelate hydrochloride

Sarpogrelate 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.

S3723

Ramosetron Hydrochloride

Ramosetron Hydrochloride is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.

S2346

Puerarin

Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.

2019, 73(6):373-382

2015, 10.1021/cb5009487

S5538

Tropisetron

Tropisetron is a 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.

S5428

Promazine hydrochloride

Promazine 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.

S4283

Cyclobenzaprine HCl

Cyclobenzaprine HCl is a muscle relaxant by blocking pain sensations, used for the treatment of muscle spasms; A 5-HT2 receptor antagonist.

S5052

Granisetron

Granisetron is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.

S2669

LY310762 HCl

LY310762 is a 5-HT1D receptor antagonist with Ki of 249 nM, having a weaker affinity for 5-HT1B receptor.

S9174

Xanthotoxol

Xanthotoxol, 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.

S5740

Palonosetron

Palonosetron 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).

S5060

Metadoxine

Metadoxine, 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
S2578

1-Phenylbiguanide

1-phenylbiguanide (PBG) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.

S1436

Tianeptine sodium

Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.

2014, 4:e411

S1432

Sumatriptan Succinate

Sumatriptan Succinate is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.

2017, 42(6):755-761

S2875

Prucalopride

Prucalopride 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

S1975

Aripiprazole

Aripiprazole 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

S1488

Naratriptan HCl

Naratriptan HCl is a triptan agent that is used for the treatment of migraine headaches.

S1607

Rizatriptan Benzoate

Rizatriptan Benzoate is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.

S1649

Zolmitriptan

Zolmitriptan is a novel and highly selective 5-HT(1B/1D) receptor agonist, used in the treatment of acute migraines.

2019, 560:294-305

S1385

Mosapride Citrate

Mosapride Citrate is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

S3180

Eletriptan HBr

Eletriptan is a selective 5-HT1B and 5-HT1D receptor agonist with Ki of 0.92 nM and 3.14 nM, respectively.

S4247

Prucalopride Succinate

Prucalopride 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)

S4259

Vilazodone HCl

Vilazodone 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

S2096

Almotriptan Malate

Almotriptan Malate 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

S5741

Quetiapine

Quetiapine 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.

S5848

Frovatriptan Succinate

Frovatriptan 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.

S6489

Lasmiditan succinate

Lasmiditan succinate is a novel, centrally acting, highly selective 5-HT(1F) receptor agonist (Ki=2.21 nM) without vasoconstrictor activity.

S5401

Tegaserod Maleate

Tegaserod 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.

S2852

BRL-54443

BRL 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.

S5153

Tetrahydroberberine

Tetrahydroberberine 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.

S5253

Cisapride

Cisapride is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.

S6324

5-Methoxytryptamine

5-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.

S3821

Nuciferine

Nuciferine 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.

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.

S4256

Buspirone HCl

Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.

2020, 30;141:111394

S4639

Brexpiprazole

Brexpiprazole 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.

S4839

Mosapride

Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.

S4751

Cisapride hydrate

Cisapride acts directly as a selective serotonin 5-HT4 receptor agonist with IC50 of 0.483 μM. And It also acts indirectly as a parasympathomimetic.

S2025

Urapidil HCl

Urapidil 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.

S4244

Serotonin HCl

Serotonin HCl is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.

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S3716

Flibanserin

Flibanserin is a nonhormonal, centrally acting molecule that acts as an agonist at postsynaptic 5-HT1A receptors and as an antagonist at 5-HT2A receptors.

S5843

Cinitapride Hydrogen Tartrate

Cinitapride 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

S5506

Vortioxetine

Vortioxetine, 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.

S5858

Vilazodone

Vilazodone 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

Lvguidingan

Lvguidingan (Anticonvulsant 7903) 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.

S3196

Azacyclonol

Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

Tags: 5-HT receptor drugs | Serotonin receptor drugs | 5-HT receptor agonist and antagonist drugs | Serotonin receptor antagonist drugs | Serotonin receptor agonist drugs | 5-HT3 receptor antagonist drugs | 5-HT receptor agonist and antagonist clinical trial | 5-HT receptor agonist and antagonist ic50 | 5-HT receptor agonist and antagonist review