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)
カタログ番号	製品カタログ	水	DMSO	アルコール
S1333	Fluoxetine (Lilly 110140) HCl	4 mg/mL	69 mg/mL	'69 mg/mL
S3913	Pimethixene maleate	<1 mg/mL	82 mg/mL	''7 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
S4053	Sertraline HCl	<1 mg/mL	69 mg/mL	'15 mg/mL
S3024	Lamotrigine	<1 mg/mL	10 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
S3183	Amitriptyline HCl	15 mg/mL	63 mg/mL	'63 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
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
S5485	Desipramine Hydrochloride	-1 mg/mL	60 mg/mL	''-1 mg/mL
S2582	Trazodone HCl	<1 mg/mL	4 mg/mL	<1 mg/mL
S5071	Duloxetine			' mg/mL
S2464	Sevoflurane			' 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
S4358	Pimozide	<1 mg/mL	92 mg/mL	''9 mg/mL
S5770	Pizotifen	<1 mg/mL	20 mg/mL	''30 mg/mL
S5185	Perospirone	<1 mg/mL	85 mg/mL	''85 mg/mL
S5197	Loxapine	<1 mg/mL	66 mg/mL	''66 mg/mL
S5949	Metoclopramide hydrochloride hydrate	71 mg/mL	71 mg/mL	''71 mg/mL
S5965	Urapidil	<1 mg/mL	77 mg/mL	''77 mg/mL
S7538	RS-102895 Hydrochloride	<1 mg/mL	85 mg/mL	'''85 mg/mL
S2698	RS-127445	<1 mg/mL	56 mg/mL	8 mg/mL
S1243	Agomelatine (S20098)	<1 mg/mL	48 mg/mL	''48 mg/mL
S1283	Asenapine maleate	<1 mg/mL	80 mg/mL	<1 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
S0313	Volinanserin	˂1 mg/mL	75 mg/mL	'75 mg/mL
S5947	Amitriptyline			' mg/mL
S0779	Pirenperone	<1 mg/mL	17 mg/mL	26 mg/mL
S5398	Nefazodone hydrochloride	-1 mg/mL	22 mg/mL	'-1 mg/mL
S2649	SB 200646	˂1 mg/mL	53 mg/mL	2 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
S2644	Lerisetron	<1 mg/mL	58 mg/mL	58 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
S5064	Lasmiditan	<1 mg/mL	75 mg/mL	''75 mg/mL
S3510	NLX-101	<1 mg/mL	79 mg/mL	''79 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
S0496	PF-04995274	<1 mg/mL	86 mg/mL	20 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 (R 51619)	<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
S0104	Pardoprunox (SLV-308) hydrochloride	<1 mg/mL	30 mg/mL	'<1 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
S2578	1-Phenylbiguanide	35 mg/mL	35 mg/mL	'17 mg/mL
S0476	SCH-23390 hydrochloride	20 mg/mL	65 mg/mL	'25 mg/mL
S8021	Vortioxetine (Lu AA21004) HBr	<1 mg/mL	76 mg/mL	'17 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
S3196	Azacyclonol	2 mg/mL	53 mg/mL	53 mg/mL
S0222	Lvguidingan	˂1 mg/mL	54 mg/mL	'54 mg/mL

亜型選択性的な製品

5-HT Receptor製品

All (127) 5-HT Receptor阻害剤(24) 5-HT Receptor活性剤(1) 5-HT Receptor拮抗剤(61) 5-HT Receptor作動薬(34) 5-HT Receptorモジュレータ(5)

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 (Lilly 110140) HCl Fluoxetine HCl (Lilly110140) is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.	FASEB J, 2021, 35(5):e21581 Sci Rep, 2021, 11(1):1250 Biomol Ther (Seoul), 2020, 28(2):202-210	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.
S3913^新	Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S1869	Dapoxetine HCl Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.
S1483	Iloperidone Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.	Sci Rep, 2018, 8(1):15753
S4053	Sertraline HCl Sertraline HCl (CP-51974-1) is a 5-HT antagonist with K_i of 13 nM.	Antimicrob Agents Chemother, 2021, AAC.01146-20 Sci Rep, 2021, 11(1):1250
S3024	Lamotrigine Lamotrigine (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.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S4064	Escitalopram Oxalate Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with K_i of 0.89 nM.
S2084	Duloxetine HCl Duloxetine HCl (LY-248686) 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).	Drug Metab Dispos, 2015, 44(3):378-88 J Pharmacol Exp Ther, 2014, 349(3):402-7 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.
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).	Environ Toxicol Chem, 2021, 10.1002/etc.5018 PLoS Pathog, 2020, 16;16(3):e1008341 Sci Rep, 2018, 8(1):15753
S9239	Isocorynoxeine Isocorynoxeine (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.
S3817	Harmine hydrochloride Harmine (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.
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.
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 (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.	Aging (Albany NY), 2021, 13(11):14729-14744 Sci Rep, 2021, 11(1):1250 Aging (Albany NY), 2020, 12(11):10147-10161
S8183	Pimavanserin Pimavanserin (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.	Mol Ther Oncolytics, 2020, 19:19-32 ACS Chem Neurosci, 2020, 11(2):173-183
S5485	Desipramine Hydrochloride Desipramine 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.
S2582	Trazodone HCl Trazodone HCl (AF-1161, KB-831) 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.
S2464	Sevoflurane Sevoflurane (Fluoromethyl) is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics.	ACS Chem Neurosci, 2021, 10.1021/acschemneuro.1c00131
S4377	Imipramine HCl Imipramine (Melipramine) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).
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 (LY 139603) 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.
S5563	Thioridazine hydrochloride Thioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent.	Cell Syst, 2019, 8(2):97-108
S4740	Sodium ferulate Sodium 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.
S2459	Clozapine Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.	Ann Neurol, 2020, 10.1002/ana.25935 BMC Evol Biol, 2018, 18(1):89 Molecules, 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	Olanzapine Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.	Pharmacol Res, 2021, 170:105714 Cell, 2020, S0092-8674(20)31394-5 Acta Pharmacol Sin, 2020, 10.1038/s41401-020-0378-6	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
S2232	Ketanserin Ketanserin (R41468) 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.	Lab Invest, 2021, 1-14 Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036 Sci Rep, 2018, 8(1):15753	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.
S4358^新	Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
S5770^新	Pizotifen Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site.
S5185^新	Perospirone Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.
S5197^新	Loxapine Loxapine (Adasuve), a typical neuroleptic, is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. Loxapine displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.
S5949^新	Metoclopramide hydrochloride hydrate Metoclopramide hydrochloride (Clorpa, Gimoti, Maxolon, Reglan) hydrate is primarily a Dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic.	Pharmazie, 2021, 76(4):172-174
S5965^新	Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
S7538^新	RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
S2698	RS-127445 RS-127445 (MT500) 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.	Lab Invest, 2021, 1-14 Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036 Front Pharmacol, 2018, 9:587
S1243	Agomelatine (S20098) Agomelatine (S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.	Sci Rep, 2018, 8(1):15753 Neuropsychiatry (London), 2018, None Arch Oral Biol, 2017, 82:11-18
S1283	Asenapine maleate Asenapine 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.	Biochem Biophys Res Commun, 2021, 553:172-179 Sci Rep, 2018, 8(1):15753
S1615	Risperidone Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.	BMC Evol Biol, 2018, 18(1):89
S1444	Ziprasidone HCl Ziprasidone HCl (CP-88059) 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, 2018, 8(1):15753 Sci Rep, 2017, 7(1):8491	a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM.
S2663	WAY-100635 Maleate WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.	Sci Rep, 2021, 11(1):9300 J Pain, 2019, 20(1):16.e1-16.e16 Neurochem Res, 2018, 43(7):1371-1382	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 (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.	Sci Rep, 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 pK_i of 8.3, exhibits >50-fold selectivity against other receptors.	J Neurotrauma, 2018, 10.1089/neu.2018.5652 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 (Org3770) is an adrenergic and seroton receptor antagonist, used to treat depression.
S2894	SB742457 SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.	Sci Rep, 2018, 8(1):15753 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.	Brain Behav Immun, 2018, 74:49-67 Anesth Analg, 2018, 10.1213/ANE.0000000000003757 Int Immunopharmacol, 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.	Clin Exp Metastasis, 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
S1390	Ondansetron HCl Ondansetron HCl (GR 38032F) is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.	Immunity, 2019, 50(5):1163-1171 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 (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.
S1394	Pizotifen Malate Pizotifen Malate (BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches.
S2106	Azasetron HCl Azasetron 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.
S4249	Flopropione Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.	Front Microbiol, 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 (GR 38032F, GR-C507/75) 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.	Sci Rep, 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
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 (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.
S4889	Perospirone hydrochloride Perospirone (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.
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 (NSC 35459) is a drug used for functional gastrointestinal disorders.	Am J Physiol Lung Cell Mol Physiol, 2018, 315(2):L133-L148
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.
S0313	Volinanserin Volinanserin (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.
S5947	Amitriptyline Amitriptyline (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. This product is a waxy solid.	Cancers (Basel), 2019, 11(12)
S0779	Pirenperone Pirenperone (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).
S5398	Nefazodone hydrochloride Nefazodone hydrochloride (BMY-13754-1) is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake.
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.
S4635	Cyproheptadine hydrochloride sesquihydrate Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.	Anticancer Res, 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 (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.	Cell, 2017, 170(1):185-198
S5714	lurasidone Lurasidone (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.
S3706	Sarpogrelate hydrochloride Sarpogrelate (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.
S3723	Ramosetron Hydrochloride Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.	Theranostics, 2020, 10(16):7351-7368
S2346	Puerarin Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.	Front Pharmacol, 2021, 12:632825 Int J Mol Sci, 2020, 21(14):5025 J Cardiovasc Pharmacol, 2019, 73(6):373-382
S5538	Tropisetron Tropisetron (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.
S2644	Lerisetron Lerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM.
S5428	Promazine hydrochloride Promazine (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.
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 (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.
S5749	Chlorpromazine Chlorpromazine (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.	Theranostics, 2021, 11(5):2364-2380 Front Oncol, 2021, 11:665832 Int J Nanomedicine, 2021, 16:2487-2499
S2669	LY310762 HCl LY310762 is a 5-HT1D receptor antagonist with K_i of 249 nM, having a weaker affinity for 5-HT1B receptor.
S9174	Xanthotoxol Xanthotoxol (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.
S5740	Palonosetron Palonosetron (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).
S5060	Metadoxine Metadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication.
S5064^新	Lasmiditan Lasmiditan (Reyvow) is a highly selective 5-hydroxytryptamine (serotonin) receptor 1F (5-HT1F) agonist that can be used as a promising acute anti-migraine therapy.
S3510^新	NLX-101 NLX-101 (F-15599) is a potent and selective activator of serotonin 5-HT1A receptor.
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 (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.	J Toxicol Sci, 2017, 42(6):755-761
S2875	Prucalopride Prucalopride (R-93877) 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.	Front Pharmacol, 2019, 10:1491 Gut, 2019, 68(8):1406-1416 Nutrients, 2017, 9(12)	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 (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.	Antimicrob Agents Chemother, 2021, AAC.01146-20 BMC Evol Biol, 2018, 18(1):89 J Psychiatr Res, 2018, 105:95-102	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 (MK-462) 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.	Int J Pharm, 2019, 560:294-305
S1385	Mosapride Citrate Mosapride Citrate (AS-4370) is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S3180	Eletriptan HBr Eletriptan (UK-116044) 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.	Front Pharmacol, 2019, 10:1491 Front Pharmacol, 2018, 9:171 Neurogastroenterol Motil, 2018, 30(2)	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.
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.	J Pain, 2019, 20(1):16.e1-16.e16 Acta Pol Pharm, 2017, 74(3):765-775
S2096	Almotriptan Malate Almotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.	Oncotarget, 2017, 9(3):3507-3518 Oncotarget, 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.
S0496	PF-04995274 PF-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.
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 (COL-144, LY573144) 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 pK_i of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.	Theranostics, 2021, 11(14):6950-6965
S5153	Tetrahydroberberine Tetrahydroberberine (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.
S5253	Cisapride (R 51619) Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
S6324	5-Methoxytryptamine 5-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.
S3821	Nuciferine Nuciferine (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.	Br J Pharmacol, 2021, 178(5):1182-1199 Tohoku J Exp Med, 2021, 254(1):17-23
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.
S0104	Pardoprunox (SLV-308) hydrochloride Pardoprunox 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.
S4256	Buspirone HCl Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.	Food Chem Toxicol, 2020, 30;141:111394
S4639	Brexpiprazole Brexpiprazole (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.
S4839	Mosapride Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S4751	Cisapride hydrate Cisapride (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.
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 (5-HT) is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.	Theranostics, 2021, 11(14):6950-6965 Sci Rep, 2021, 11(1):1250
S2578	1-Phenylbiguanide 1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.
S0476	SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) 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.
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.
S3716	Flibanserin Flibanserin (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.
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 (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.	J Pain, 2019, 20(1):16.e1-16.e16
S3196	Azacyclonol Azacyclonol (MER 17, MDL 4829), also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.	Oncol Rep, 2020, 44(6):2503-2516
S0222	Lvguidingan Lvguidingan (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.

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 (Lilly 110140) HCl Fluoxetine HCl (Lilly110140) is a selective serotonin-reuptake inhibitor (SSRI) at the neuronal membrane, used in the treatment of depression.	FASEB J, 2021, 35(5):e21581 Sci Rep, 2021, 11(1):1250 Biomol Ther (Seoul), 2020, 28(2):202-210	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.
S3913^新	Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.
S1869	Dapoxetine HCl Dapoxetine HCl (LY-210448) is a short-acting novel selective serotonin reuptake inhibitor, used for the treatment of premature ejaculation.
S1483	Iloperidone Iloperidone (HP873) is a dopamine (D2)/serotonin (5-HT2) receptor antagonist, used for the treatment of schizophrenia.	Sci Rep, 2018, 8(1):15753
S4053	Sertraline HCl Sertraline HCl (CP-51974-1) is a 5-HT antagonist with K_i of 13 nM.	Antimicrob Agents Chemother, 2021, AAC.01146-20 Sci Rep, 2021, 11(1):1250
S3024	Lamotrigine Lamotrigine (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.	Cancer Cell Int, 2020, 19;20:58 Hum Cell, 2020, 10.1007/s13577-020-00425-8 Hum Cell, 2020, 10.1007/s13577-020-00420-z
S4064	Escitalopram Oxalate Escitalopram Oxalate is a selective serotonin (5-HT) reuptake inhibitor (SSRI) with K_i of 0.89 nM.
S2084	Duloxetine HCl Duloxetine HCl (LY-248686) 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).	Drug Metab Dispos, 2015, 44(3):378-88 J Pharmacol Exp Ther, 2014, 349(3):402-7 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.
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).	Environ Toxicol Chem, 2021, 10.1002/etc.5018 PLoS Pathog, 2020, 16;16(3):e1008341 Sci Rep, 2018, 8(1):15753
S9239	Isocorynoxeine Isocorynoxeine (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.
S3817	Harmine hydrochloride Harmine (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.
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.
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 (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.	Aging (Albany NY), 2021, 13(11):14729-14744 Sci Rep, 2021, 11(1):1250 Aging (Albany NY), 2020, 12(11):10147-10161
S8183	Pimavanserin Pimavanserin (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.	Mol Ther Oncolytics, 2020, 19:19-32 ACS Chem Neurosci, 2020, 11(2):173-183
S5485	Desipramine Hydrochloride Desipramine 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.
S2582	Trazodone HCl Trazodone HCl (AF-1161, KB-831) 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.
S2464	Sevoflurane Sevoflurane (Fluoromethyl) is a noncompetitive inhibitor of 5-HT3 receptor. Sevoflurane acts as a low-soluble inhalation anesthetics.	ACS Chem Neurosci, 2021, 10.1021/acschemneuro.1c00131
S4377	Imipramine HCl Imipramine (Melipramine) is a tricyclic antidepressant (TCA) of the dibenzazepine group, mainly used in the treatment of major depression and enuresis (inability to control urination).
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 (LY 139603) 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.
S5563	Thioridazine hydrochloride Thioridazine (Aldazine, Mellaril) is a potent antianxiety and antipsychotic agent.	Cell Syst, 2019, 8(2):97-108

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S4740	Sodium ferulate Sodium 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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S4740

Sodium ferulate

Sodium 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
S2459	Clozapine Clozapine (HF 1854, LX 100-129) is an atypical antipsychotic drug by acting as a 5-HT antagonist, used in the treatment of schizophrenia.	Ann Neurol, 2020, 10.1002/ana.25935 BMC Evol Biol, 2018, 18(1):89 Molecules, 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	Olanzapine Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.	Pharmacol Res, 2021, 170:105714 Cell, 2020, S0092-8674(20)31394-5 Acta Pharmacol Sin, 2020, 10.1038/s41401-020-0378-6	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
S2232	Ketanserin Ketanserin (R41468) 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.	Lab Invest, 2021, 1-14 Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036 Sci Rep, 2018, 8(1):15753	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.
S4358^新	Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
S5770^新	Pizotifen Pizotifen (Pizotyline, BC-105) is a potent antagonist of 5-Hydroxytryptamine (5-HT, Serotonin) 5-HT2 receptor with a high affinity for 5-HT1C binding site.
S5185^新	Perospirone Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.
S5197^新	Loxapine Loxapine (Adasuve), a typical neuroleptic, is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. Loxapine displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.
S5949^新	Metoclopramide hydrochloride hydrate Metoclopramide hydrochloride (Clorpa, Gimoti, Maxolon, Reglan) hydrate is primarily a Dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic.	Pharmazie, 2021, 76(4):172-174
S5965^新	Urapidil Urapidil is an antihypertensive drug acting as an α1 adrenoreceptor antagonist and a 5-HT1A agonist.
S7538^新	RS-102895 Hydrochloride RS-102895 hydrochloride (HCl) is a potent antagonist of Chemokine (C-C motif) receptor 2 (CCR2) with IC50 of 360 nM, and shows no effect on CCR1. RS-102895 hydrochloride also inhibits human α1a and α1d receptors, rat brain cortex 5-HT1a receptor in cells with IC50s of 130 nM, 320 nM, 470 nM, respectively.
S2698	RS-127445 RS-127445 (MT500) 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.	Lab Invest, 2021, 1-14 Int Immunopharmacol, 2019, 10.1016/j.intimp.2019.106036 Front Pharmacol, 2018, 9:587
S1243	Agomelatine (S20098) Agomelatine (S20098) is classified as a norepinephrine-dopamine disinhibitor (NDDI) due to its antagonism of the 5-HT2C receptor.	Sci Rep, 2018, 8(1):15753 Neuropsychiatry (London), 2018, None Arch Oral Biol, 2017, 82:11-18
S1283	Asenapine maleate Asenapine 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.	Biochem Biophys Res Commun, 2021, 553:172-179 Sci Rep, 2018, 8(1):15753
S1615	Risperidone Risperidone (R-64766) is a mutil-targeted antagonist for dopamine, serotonin, adrenergic and histamine receptors, used to treat schizophrenia and bipolar disorder.	BMC Evol Biol, 2018, 18(1):89
S1444	Ziprasidone HCl Ziprasidone HCl (CP-88059) 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, 2018, 8(1):15753 Sci Rep, 2017, 7(1):8491	a, Quantification of sterol levels in OPCs (oligodendrocyte progenitor cells) treated with the indicated molecules at 2 μM.
S2663	WAY-100635 Maleate WAY-100635 Maleate is a potent and selective 5-HT receptor antagonist with IC50 of 0.95 nM.	Sci Rep, 2021, 11(1):9300 J Pain, 2019, 20(1):16.e1-16.e16 Neurochem Res, 2018, 43(7):1371-1382	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 (AD 5423) is a relatively selective serotonin (5-HT)2A and dopamine D2 antagonist, used the treatment of schizophrenia.	Sci Rep, 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 pK_i of 8.3, exhibits >50-fold selectivity against other receptors.	J Neurotrauma, 2018, 10.1089/neu.2018.5652 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 (Org3770) is an adrenergic and seroton receptor antagonist, used to treat depression.
S2894	SB742457 SB742457 (GSK 742457) is a highly selective 5-HT6 receptor antagonist with pKi of 9.63, exhibits >100-fold selectivity over other receptors. Phase 2.	Sci Rep, 2018, 8(1):15753 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.	Brain Behav Immun, 2018, 74:49-67 Anesth Analg, 2018, 10.1213/ANE.0000000000003757 Int Immunopharmacol, 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.	Clin Exp Metastasis, 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
S1390	Ondansetron HCl Ondansetron HCl (GR 38032F) is a serotonin 5-HT3 receptor antagonist, used to prevent nausea and vomiting caused by cancer chemotherapy, and radiation therapy.	Immunity, 2019, 50(5):1163-1171 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 (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.
S1394	Pizotifen Malate Pizotifen Malate (BC-105) is a benzocycloheptane based agent used for recurrent migraine headaches.
S2106	Azasetron HCl Azasetron 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.
S4249	Flopropione Flopropione is a spasmolytic or antispasmodic agent, and acts as a 5-HT1A receptor antagonist.	Front Microbiol, 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 (GR 38032F, GR-C507/75) 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.	Sci Rep, 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
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 (RS 25259, RS 25259 197) is a 5-HT3 antagonist used in the prevention and treatment of chemotherapy-induced nausea and vomiting.
S4889	Perospirone hydrochloride Perospirone (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.
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 (NSC 35459) is a drug used for functional gastrointestinal disorders.	Am J Physiol Lung Cell Mol Physiol, 2018, 315(2):L133-L148
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.
S0313	Volinanserin Volinanserin (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.
S5947	Amitriptyline Amitriptyline (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. This product is a waxy solid.	Cancers (Basel), 2019, 11(12)
S0779	Pirenperone Pirenperone (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).
S5398	Nefazodone hydrochloride Nefazodone hydrochloride (BMY-13754-1) is the hydrochloride salt form of nefazodone, which is an atypical antidepressant showing antagonistic activity on serotonin reuptake.
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.
S4635	Cyproheptadine hydrochloride sesquihydrate Cyproheptadine hydrochloride (Periactin, Peritol) is non-selective 5HT2 antagonist with IC50 of 0.6 nM. Also a SETD7/9 inhibitor.	Anticancer Res, 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 (GR 68755C, GR 68755X, Lotronex) is the hydrochloride salt form of alosetron, a potent and selective 5-HT3 receptor antagonist.	Cell, 2017, 170(1):185-198
S5714	lurasidone Lurasidone (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.
S3706	Sarpogrelate hydrochloride Sarpogrelate (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.
S3723	Ramosetron Hydrochloride Ramosetron Hydrochloride (YM-060) is the hydrochloride salt of ramosetron, a selective serotonin (5-HT) receptor antagonist with potential antiemetic activity.	Theranostics, 2020, 10(16):7351-7368
S2346	Puerarin Puerarin (Kakonein), an isoflavones found in the root of Radix puerariae, is a 5-HT2C receptor and benzodiazepine site antagonist.	Front Pharmacol, 2021, 12:632825 Int J Mol Sci, 2020, 21(14):5025 J Cardiovasc Pharmacol, 2019, 73(6):373-382
S5538	Tropisetron Tropisetron (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.
S2644	Lerisetron Lerisetron (F 0930, F 0930RS) is a 5-HT3 receptor antagonist with IC50 of 0.81μM.
S5428	Promazine hydrochloride Promazine (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.
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 (Sancuso, Kevatril, Granisetronum, Sustol) is a serotonin receptor (5HT-3 selective) antagonist that is used as an antiemetic and antinauseant for cancer chemotherapy.
S5749	Chlorpromazine Chlorpromazine (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.	Theranostics, 2021, 11(5):2364-2380 Front Oncol, 2021, 11:665832 Int J Nanomedicine, 2021, 16:2487-2499
S2669	LY310762 HCl LY310762 is a 5-HT1D receptor antagonist with K_i of 249 nM, having a weaker affinity for 5-HT1B receptor.
S9174	Xanthotoxol Xanthotoxol (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.
S5740	Palonosetron Palonosetron (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).
S5060	Metadoxine Metadoxine (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
S5064^新	Lasmiditan Lasmiditan (Reyvow) is a highly selective 5-hydroxytryptamine (serotonin) receptor 1F (5-HT1F) agonist that can be used as a promising acute anti-migraine therapy.
S3510^新	NLX-101 NLX-101 (F-15599) is a potent and selective activator of serotonin 5-HT1A receptor.
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 (GR 43175) is a triptan sulfa drug containing a sulfonamide group for the treatment of migraine headaches.	J Toxicol Sci, 2017, 42(6):755-761
S2875	Prucalopride Prucalopride (R-93877) 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.	Front Pharmacol, 2019, 10:1491 Gut, 2019, 68(8):1406-1416 Nutrients, 2017, 9(12)	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 (OPC-14597) is a novel atypical antipsychotic drug that is reported to be a high-affinity 5-HT receptor partial agonist.	Antimicrob Agents Chemother, 2021, AAC.01146-20 BMC Evol Biol, 2018, 18(1):89 J Psychiatr Res, 2018, 105:95-102	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 (MK-462) 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.	Int J Pharm, 2019, 560:294-305
S1385	Mosapride Citrate Mosapride Citrate (AS-4370) is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S3180	Eletriptan HBr Eletriptan (UK-116044) 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.	Front Pharmacol, 2019, 10:1491 Front Pharmacol, 2018, 9:171 Neurogastroenterol Motil, 2018, 30(2)	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.
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.	J Pain, 2019, 20(1):16.e1-16.e16 Acta Pol Pharm, 2017, 74(3):765-775
S2096	Almotriptan Malate Almotriptan Malate (LAS 31416) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.	Oncotarget, 2017, 9(3):3507-3518 Oncotarget, 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.
S0496	PF-04995274 PF-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.
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 (COL-144, LY573144) 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 pK_i of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.	Theranostics, 2021, 11(14):6950-6965
S5153	Tetrahydroberberine Tetrahydroberberine (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.
S5253	Cisapride (R 51619) Cisapride (R 51619, Kaudalit, Kinestase, Prepulsid, Presid, Pridesia, Propulsid) is a nonselective 5-HT4 receptor agonist with gastroprokinetic effects.
S6324	5-Methoxytryptamine 5-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.
S3821	Nuciferine Nuciferine (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.	Br J Pharmacol, 2021, 178(5):1182-1199 Tohoku J Exp Med, 2021, 254(1):17-23
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.
S0104	Pardoprunox (SLV-308) hydrochloride Pardoprunox 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.
S4256	Buspirone HCl Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders.	Food Chem Toxicol, 2020, 30;141:111394
S4639	Brexpiprazole Brexpiprazole (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.
S4839	Mosapride Mosapride is a gastroprokinetic agent that acts as a selective 5HT4 agonist.
S4751	Cisapride hydrate Cisapride (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.
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 (5-HT) is a monoamine neurotransmitter and Endogenous 5-HT receptor agonist.	Theranostics, 2021, 11(14):6950-6965 Sci Rep, 2021, 11(1):1250
S2578	1-Phenylbiguanide 1-Phenylbiguanide (Phenylbiguanide, PBG, N-Phenylbiguanide) is a 5-hydroxytryptamine3 (5-HT3) receptor agonist with EC50 of 3.0 μM.
S0476	SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) 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.

製品コード	製品説明	文献中Selleckの製品使用例
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.
S3716	Flibanserin Flibanserin (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.
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 (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.	J Pain, 2019, 20(1):16.e1-16.e16

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
S3196	Azacyclonol Azacyclonol (MER 17, MDL 4829), also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.	Oncol Rep, 2020, 44(6):2503-2516
S0222	Lvguidingan Lvguidingan (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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文献中Selleckの製品使用例

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S3196

Azacyclonol

Azacyclonol (MER 17, MDL 4829), also known as γ-pipradol, is a drug used to diminish hallucinations in psychotic individuals.

Oncol Rep, 2020, 44(6):2503-2516

S0222

Lvguidingan

Lvguidingan (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.