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
溶解度

カタログ番号	製品カタログ	溶解度(25°C)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1333	Fluoxetine HCl	4 mg/mL	69 mg/mL	69 mg/mL
S5693	Levomilnacipran Hydrochloride	-1 mg/mL	57 mg/mL	-1 mg/mL
S9039	Albiflorin		96 mg/mL
S5655	Venlafaxine	<1 mg/mL	55 mg/mL	<1 mg/mL
S5239	Paroxetine mesylate	-1 mg/mL	85 mg/mL	-1 mg/mL
S5485	Desipramine Hydrochloride	-1 mg/mL	60 mg/mL	-1 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
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
S1642	Methyldopa	<1 mg/mL	2 mg/mL	<1 mg/mL
S8183	Pimavanserin	100 mg/mL	100 mg/mL	100 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
S3175	Atomoxetine HCl	2 mg/mL	58 mg/mL	37 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
S5398	Nefazodone hydrochloride	-1 mg/mL	22 mg/mL	-1 mg/mL
S5714	lurasidone	<1 mg/mL	7 mg/mL	<1 mg/mL
S5326	Dolasetron	<1 mg/mL	64 mg/mL	<1 mg/mL
S5153	Tetrahydroberberine	-1 mg/mL	6 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
S4889	Perospirone hydrochloride	-1 mg/mL	92 mg/mL	-1 mg/mL
S5052	Granisetron	-1 mg/mL	11 mg/mL	-1 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
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
S3050	Palonosetron HCl	67 mg/mL	<1 mg/mL	<1 mg/mL
S2865	VUF 10166	<1 mg/mL	21 mg/mL	61 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
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
S4283	Cyclobenzaprine HCl	62 mg/mL	62 mg/mL	62 mg/mL
S2669	LY310762 HCl	<1 mg/mL	0.4 mg/mL	<1 mg/mL
S5401	Tegaserod Maleate	<1 mg/mL	83 mg/mL	8 mg/mL
S5253	Cisapride	<1 mg/mL	93 mg/mL	<1 mg/mL
S4839	Mosapride	-1 mg/mL	84 mg/mL	-1 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
S2096	Almotriptan Malate	<1 mg/mL	94 mg/mL	53 mg/mL
S2852	BRL-54443	<1 mg/mL	46 mg/mL	2 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
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
S5506	Vortioxetine	<1 mg/mL	34 mg/mL	28 mg/mL
S3716	Flibanserin	<1 mg/mL	78 mg/mL	23 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阻害剤(95)
新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.	G3 (Bethesda), 2014, 4(6):1081-9 Georgia State University, 2014, Chaquettea Felton	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.
S5693^新	Levomilnacipran Hydrochloride Levomilnacipran Hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor with antidepressant activity.
S9510^新	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.
S9258^新	(+)-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.
S9039^新	Albiflorin Albiflorin, a natural product isolated from Paeoniae Radix, is a novel 5-HT and NE reuptake inhibitor with high selectivity.
S5655^新	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.
S5239^新	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.
S5485^新	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.
S5071^新	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.
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) is a multimodal serotonergic agent, inhibits 5-HT1A, 5-HT1B, 5-HT3A, 5-HT7 receptor and SERT with IC50 of 15 nM, 33 nM, 3.7 nM, 19 nM and 1.6 nM, respectively.
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 K_i 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 K_i of 40.2 nM and 558.4 nM, respectively.
S2084	Duloxetine HCl Duloxetine HCl is a serotonin-norepinephrine reuptake inhibitor with K_i of 4.6 nM, used for treatment of major depressive disorder and generalized anxiety disorder (GAD).	J Pharmacol Exp Ther, 2014, 349(3):402-7 Drug Metab Dispos, 2015, 44(3):378-88 Am J Physiol Renal Physiol, 2013, 305(12):F1663-8	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.
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 inhibits serotonin receptor, norepinephrine receptor, 5-HT4, 5-HT2 and sigma 1 receptor with IC50 of 3.45 nM, 13.3 nM, 7.31 nM, 235 nM and 287 nM, respectively.
S1642	Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
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.
S4112	Desvenlafaxine Succinate Desvenlafaxine Succinate is a new serotonin (5-HT) transporter and norepinephrine (NE) transporter reuptake inhibitor with K_i 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.
S3175	Atomoxetine HCl Atomoxetine is a selective norepinephrine (NE) transporter inhibitor with K_i of 5 nM, with 15- and 290-fold lower affinity for human 5-HT and DA transporters.
S2459	Clozapine Clozapine is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.	Drug Metab Dispos, 2015, 43(7):1147-53	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	Olanzapine Olanzapine is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.	J Psychiatr Res, 2017, 88:18-27 Asian Pac J Cancer Prev, 2014, 15(19):8107-13	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 ¼ 4e6 independent cell isolations measured in duplicate.
S2232	Ketanserin Ketanserin is a specific 5-HT2A serotonin receptor antagonist with K_i 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.
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.
S5398^新	Nefazodone hydrochloride Nefazodone hydrochloride is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake.
S5740^新	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).
S9174^新	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.
S5714^新	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.
S5326^新	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.
S5153^新	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.
S5538^新	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^新	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.
S4889^新	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.
S5052^新	Granisetron Granisetron is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.
S2698	RS-127445 RS-127445 is a selective 5-HT2B receptor antagonist with pK_i 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.	Nature, 2018, 560(7718):372-376 Sci Rep, 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.	PLoS One, 2017, 12(1):e0168964 Sci Rep, 2014, 4:7270	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	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 pK_i of 8.3, exhibits >50-fold selectivity against other receptors.	Sci Rep, 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 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.	Sci Rep, 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
S2677	BRL-15572(dihydrochloride) BRL-15572 is a 5-HT1D receptor antagonist with pK_i of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.
S1390	Ondansetron HCl Ondansetron is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.	Int J Urol, 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.
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.	Int J Urol, 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.
S2856	SB 271046 hydrochloride SB 271046 hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pK_i 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
S3050	Palonosetron HCl Palonosetron HCl is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.
S2865	VUF 10166 VUF10166 is a novel, potent and competitive antagonist for 5-HT3A receptor with K_i of 0.04 nM, its affinity at 5-HT3AB receptor is significantly lower.
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.
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.	ACS Chem Biol, 2015, 10.1021/cb5009487
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.
S2669	LY310762 HCl LY310762 is a 5-HT1D receptor antagonist with K_i of 249 nM, having a weaker affinity for 5-HT1B receptor.
S5401^新	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.
S5253^新	Cisapride Cisapride is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
S4839^新	Mosapride Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S1436	Tianeptine sodium Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE), used for treating major depressive episodes.	Transl Psychiatry, 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.
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 K_i of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.	Neurogastroenterol Motil, 2017, 10.1111/nmo.13064 Neurogastroenterol Motil, 2016, 28(8):1241-51	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	Aripiprazole Aripiprazole is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.	J Psychiatr Res, 2017, 88:18-27	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
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 K_i 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.	Neurogastroenterol Motil, 2017, 29(8)
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.	Oncotarget, 2016, 7(9):9975-92
S2852	BRL-54443 BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pK_i of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
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.
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.
S5506^新	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.
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.
S3196	Azacyclonol Azacyclonol, also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

研究分野別

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5-HT受容体

シグナル伝達経路

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