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5-HT Receptor agonist
Clomipramine is a blocker of the following transporters:Serotonin transporter (SERT) (Ki = 0.14 nM),Norepinephrine transporter (NET) (Ki = 54 nM),Dopamine transporter (DAT) (Ki = 3,020 nM),Glycine transporter (GlyT/LeuT). -
5-HT4-receptor agonist
Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist. -
5-HT Receptor agonist
Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE) in vitro and in vivo. -
5-HT1B/1D receptor agonist
Eletriptan hydrobromide is a selective SR-1B/SR-1D agonist.- Li Li, .et al. , J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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5-HT Receptor agonist
Prucalopride is a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements.- Pierre Meschin, .et al. , Cell Calcium, 2015, Dec;58(6):549-57 PMID: 26427584
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5-HT Receptor agonist
Almotriptan malate (Axert) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.- Li Li, .et al. , J Exp Med, 2022, Aug 1;219(8):e20212307 PMID: 35796804
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5-HT1A receptor agonist
Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.- Jaime Osuna-Luque, .et al. , J Exp Neurosci, 2018, 12: 1179069518798628 PMID: 30245571
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5-HT2c receptor agonist
PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1. -
5-HT1A receptor agonist
Lesopitron dihydrochloride is a full and selective 5-HT1A receptor agonist with IC50 of 125 nM in rat hippocampal membranes. -
5-HT1B/1D receptors agonist
Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively. -
5-HT2C agonist
S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors). -
5-HT1A/1B and 5-HT2C agonist
RU 24969 hemisuccinate is a potent 5-HT1A/1B and moderate 5-HT2C agonist that may also release 5-HT. -
5-HT6 agonist
WAY 181187 is a high affinity and selective 5-HT6 agonist with Ki value of 2.2 nM. -
5-HT2A receptor agonist
Pimavanserin is a potent and selective 5-HT2A receptor inverse agonist with mean pIC50 of with 8.7 in the cell-based functional assay. -
5HT(1A) receptor agonist
Buspirone is a serotonergic (5HT(1A) receptor agonist) anxiolytic drug with some D(2) dopaminergic effect, used for anxiety disorders. -
Serotonin2A Receptor Inverse Agonist
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. -
5HT(1A) receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. -
5-HT1A receptor agonist/serotonin reuptake inhibitor
YL0919, a novel antidepressant candidate with dual activity as a 5-HT1A receptor agonist and a selective serotonin reuptake inhibitor,the IC50 values of YL-0919 inhibiting the uptake of 5-HT into rat cerebral cortical synaptosomes and human recombinant cells were 1.78??0.34 nM and 1.93??0.18 nM respectively. -
5-HT(2A) receptor agonist
Temanogrel, also known as APD791, is a highly selective 5-hydroxytryptamine2A receptor inverse agonist under development for the treatment of arterial thrombosis. -
Serotonin receptors agonist
Dihydroergotamine Mesylate, also known as DHE or Migranal, is an ergot alkaloid used to treat migraines. It has similar actions to the triptans, acting as an agonist to the serotonin receptors and causing vasoconstriction of the intracranial blood vessels, but also interacts centrally with dopamine and adrenergic receptors. -
5-HT1A receptor agonist
Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential. The affinity of F 11440 for 5-HT1A binding sites (pKi, 8.33) was higher than that of buspirone (pKi, 7.50), and somewhat lower than that of flesinoxan (pKi, 8.91). In vivo, F 11440 was 4- to 20-fold more potent than flesinoxan, and 30- to 60-fold more potent than buspirone. -
5-HT2C receptor-selective agonist
Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM. -
5-HT6 agonist
EMDT oxalate is a selective 5-HT6 agonist, and has antidepressant effects. -
5-HT7 receptor agonist
5-HT7 agonist 1 is a selective 5-HT7 receptor agonist, with an IC50 of 222.93 nM, can be used for the 5-HT7 receptor related disease, such as CNS disorders. -
5-HT3 partial agonist
Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease. -
5-HT3 receptor selective agonist
Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM. -
5-HT1A/5-HT1B/5-HT1C agonist
Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor. -
5-HT(2C) receptor agonist
WAY 163909 is a potent and selective 5-HT(2C) receptor agonist with a Ki of 10.5??1.1 nM. -
5-HT2A inverse agonist
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively. -
5-HT1F receptor agonist
LY 344864 S-enantiomer is the S-enantiomer of LY344864. LY344864 is a 5-HT1F receptor agonist. -
5-HT1F agonist
LY 344864 hydrochloride is a selective 5-HT1F agonist with a Ki of 6 nM. -
SSR inhibitor / 5-HT1A receptor partial agonist
Vilazodone D8 is the a deuterium labeled vilazodone, which is a combined serotonin specific reuptake inhibitor (SSRI) and 5-HT1A receptor partial agonist. -
human 5-HT1A receptor partial agonist
Aripiprazole D8 (OPC-14597 D8) is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM. -
5-HT4 receptor partial agonist
PF-04995274 is a partial agonist of the serotonin (5-HT) receptor subtypes 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E (Kis = 0.36, 0.46, 0.15, and 0.32 nM, respectively, in a radioligand binding assay).1 It increases cAMP levels in HEK293 cells expressing 5-HT4A, 5-HT4B, 5-HT4D, and 5-HT4E receptors (EC50s = 0.47, 0.36, 0.37, and 0.26 nM, respectively, for the human recombinant receptors). PF-04995274 decreases scopolamine-induced increases in the distance traveled in the Morris water maze in rats when administered at a dose of 0.032 mg/kg. -
5-HT receptor agonist
MK 212 hydrochloride is a 5-HT receptor agonist; displays selectivity for 5-HT2C over 5-HT2A (IC50 values are 0.028 and 0.42 μM for human 5-HT2C and 5-HT2A receptors expressed in HEK293 cells respectively). -
5-HT receptor agonist
Quipazine maleate is a selective 5-HT receptor agonist that promotes the proliferation and apoptosis of human hepatocyte strain of L-02 strain and could also exert an excitatory effect on raphe neurons via stimulation of 5-HT2A receptors.