5-HT Receptor
Serotonin Receptor; 5-hydroxytryptamine Receptor
5-HT receptors (Serotonin receptors) are a group of G protein-coupled receptors (GPCRs) and ligand-gated ion channels (LGICs) found in the central and peripheral nervous systems. Type: 5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7. They mediate both excitatory and inhibitory neurotransmission. The serotonin receptors are activated by the neurotransmitter serotonin, which acts as their natural ligand. The serotonin receptors modulate the release of many neurotransmitters, as well as many hormones. The serotonin receptors influence various biological and neurological processes such as aggression, anxiety, appetite, cognition, learning, memory, mood, nausea, sleep, andthermoregulation. The serotonin receptors are the target of a variety of pharmaceutical drugs, including many antidepressants, antipsychotics, anorectics,antiemetics, gastroprokinetic agents, antimigraine agents, hallucinogens, and entactogens.
5-HT Receptor Isoform Specific Products
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5-HT Receptor
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5-HT1 Receptor
(448)
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5-HT2 Receptor
(475)
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5-HT3 Receptor
(31)
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5-HT4 Receptor
(12)
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5-HT5 Receptor
(12)
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5-HT6 Receptor
(85)
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5-HT7 Receptor
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All Product Categories
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5-HT Receptor Inhibitors
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5-HT Receptor Agonists
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5-HT Receptor Antagonists
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5-HT Receptor Activators
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5-HT Receptor Modulators
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5-HT Receptor Inducers
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5-HT Receptor Controls
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5-HT Receptor Ligands
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5-HT Receptor Related Products (1722)
Related Products (1722)
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Antibodies (1)
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Related Compound Screening Libraries (1)
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5-HT Receptor Isoform Comparison
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VUF10166
0 ImagesVUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM.
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Relenopride hydrochloride
0 ImagesSynonyms: YKP10811 hydrochlorideRelenopride (YKP10811) hydrochloride is a specific and selective 5-HT4 receptor agonist (Ki=4.96 nM). Relenopride hydrochloride has 120-fold and 6-fold lower affinity, respectively, for 5-HT2A (Ki=600 nM) and 5-HT2B receptors (Ki=31 nM) than for 5-HT4. Relenopride hydrochloride increases gastrointestinal (GI) motility.
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ARC 239
0 ImagesARC 239 is an α2B/C-adrenergic receptor antagonist with pKi of 7.06 and 6.95 for rat kidney α2B and human α2C, respectively. ARC 239 also inhibits 5-HT1A receptor with a Ki of 63.1 nM.
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5-HT2C agonist-3
0 Images5-HT2C agonist-3 ((+)-19) is a selective 5-HT2C agonist (EC50: 24 nM, Ki: 78 nM). 5-HT2C agonist-3 has antipsychotic drug-like activity. 5-HT2C agonist-3 blocks Amphetamine-induced hyperactivity.
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Sumatriptan-d6 succinate
0 ImagesSynonyms: GR 43175C-d6Sumatriptan-d6 succinate is the deuterium labeled Sumatriptan succinate. Sumatriptan succinate is an orally active 5-HT1 receptor agonist with Kis of 17 nM, 27 nM and 100 nM for 5-HT1D, 5-HT1B and 5-HT1A receptors, respectively. Sumatriptan succinate can be used for migraine headache research.
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Mosapramine
0 ImagesSynonyms: ClospipramineMosapramine (Clospipramine) is an orally active antipsychotic agent and one of the metabolites of Clocapramine (HY-B2073) after oral absorption. Mosapramine exerts its effects by specifically binding to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, with a D2/5-HT2 receptor occupancy ratio of 7.4. Mosapramine induces typical neuropharmacological responses in rat brain regions, including extrapyramidal symptoms, hyperprolactinemia, increased salivation, constipation, and upregulated Fos protein expression. Mosapramine also features a reduced incidence of weight loss. Mosapramine is applicable to research related to schizophrenia.
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ST1936
0 ImagesST1936 is a selective, nanomolar affinity 5-HT6 receptor agonist with Ki values of 13 nM, 168 nM and 245 nM for human 5-HT6, 5-HT7 and 5-HT2B receptors, respectively. ST1936 also shows moderate affinity (Ki of 300 nM) for human and rat α2 adrenergic receptor.
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Spiramide
0 ImagesSpiramide (AMI-193) is a potent and selective antagonist of 5-HT2 and dopamine D2 receptor, with Kis of 2 nM and 3 nM, respectively. Spiramide has >2000-fold selectivity for 5-HT2 versus 5-HT1C (Ki=4300 nM) receptors. Spiramide exhibits antipsychotic activity.
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(S)-Mirtazapine
0 ImagesSynonyms: (S)-Org3770; (S)-6-Azamianserin
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cis-(Z)-Flupentixol dihydrochloride
0 ImagesCat. No.: HY-15856CAS No.: 51529-01-2Synonyms: cis-(Z)-Flupenthixol dihydrochloridecis-(Z)-Flupentixol dihydrochloride is a potent and selective DA D1/D2 receptor antagonist, with Ki values of 0.38 nM and 7 nM for D2 receptor and 5-HT2A, respectively.
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Cerlapirdine
0 ImagesSynonyms: SAM-531; PF-05212365Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.
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Brexpiprazole S-oxide
0 ImagesCat. No.: HY-133152CAS No.: 1191900-51-2Synonyms: DM-3411Brexpiprazole S-oxide (DM-3411) is a main metabolite of Brexpiprazole and is metabolized by cytochrome P450 3A4 (CYP3A4). Brexpiprazole is an atypical antipsychotic agent and a partial agonist of human 5-HT1A and dopamine receptor with Kis of 0.12 nM and 0.3 nM, respectively. Brexpiprazole is also a 5-HT2A receptor antagonist with a Ki of 0.47 nM.
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Landipirdine
0 ImagesSynonyms: RO5025181; SYN120Landipirdine (RO5025181; SYN120) is an orally active 5-HT6 and 5-HT2A receptors antagonist. Landipirdine can be used for the study of Parkinson disease.
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25N-NBOMe hydrochloride
0 Images25N-NBOMe hydrochloride, a 2C-N derivative, is a 5-HT2A and 5-HT2C receptors agonist with Ki values of 0.144 nM and 1.06 nM, respectively. 25N-NBOMe hydrochloride has little to no efficacy at inducing release of preloaded neurotransmitter from recombinant dopamine, serotonin and norepinephrine transporters.
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Ziprasidone amino acid
0 ImagesSynonyms: Ziprasidone Impurity C; Ziprasidone open ring impurityZiprasidone amino acid (Ziprasidone Impurity C) is an impurity of Ziprasidone. Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone exhibits potent effects of antipsychotic activity .
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Prucalopride-13C,d3
0 ImagesPrucalopride-13C,d3 is the 13C- and deuterium labeled Prucalopride.
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Ondansetron-d3 hydrochloride
0 ImagesOndansetron-d3 (hydrochloride) is the deuterium labeled Ondansetron hydrochloride. Ondansetron hydrochloride (GR 38032 hydrochloride) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
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LY 344864 racemate
0 ImagesCat. No.: HY-13788CCAS No.: 186543-64-6LY 344864 racemate is a 5-HT1F receptor agonist extracted from patent US 5708187 A.
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Renzapride
0 ImagesSynonyms: BRL 24924Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study.
