1. Signaling Pathways
  2. GPCR/G Protein
    Neuronal Signaling
  3. 5-HT Receptor

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-133111S
    3-Hydroxy agomelatine-d3
    Antagonist 99.92%
    3-Hydroxy agomelatine-d3 is a deuterium labeled 3-Hydroxy agomelatine. 3-Hydroxy agomelatine is a 5-HT2C receptor antagonist with an IC50 of 3.2 μM and a Ki of 1.8 μM.
    3-Hydroxy agomelatine-d<sub>3</sub>
  • HY-116594
    OPC-14523 free base
    Agonist
    OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity.
    OPC-14523 free base
  • HY-12959
    Repinotan
    Agonist
    Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.
    Repinotan
  • HY-112390
    Syk Inhibitor II dihydrochloride
    Inhibitor
    Syk Inhibitor II dihydrochloride is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II dihydrochloride inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II dihydrochloride shows less potent against other kinases and has anti-allergic effect.
    Syk Inhibitor II dihydrochloride
  • HY-B0352B
    (R)-Mirtazapine
    Antagonist 99.79%
    (R)-Mirtazapine ((R)-Org3770) is a R( )-enantiomer of Mirtazapine with antinociceptive properties in an animal model of acute thermal nociception. (R)-Mirtazapine is a 5-HT3 receptor antagonist. (R)-Mirtazapine is mainly metabolized by CYP3A4.
    (R)-Mirtazapine
  • HY-135555
    5-Carboxamidotryptamine
    Agonist 98.74%
    5-Carboxamidotryptamine (5-CT) is a 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, 5-HT7 receptor agonist. 5-Carboxamidotryptamine has a Ki value of 4.6 nM for cloned human 5-HT5A receptor. 5-Carboxamidotryptamine causes a dose-dependent reduction in rectal temperature of mice.
    5-Carboxamidotryptamine
  • HY-14441
    ML 10302
    Agonist 98.95%
    ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases.
    ML 10302
  • HY-155672
    JPC0323
    Modulator 99.5%
    JPC0323 is a dual 5-HT2C/5-HT2A receptor positive allosteric modulator. JPC0323 has on-target properties, acceptable plasma exposure and brain penetration. JPC0323 can be used for the research of neurological disease.
    JPC0323
  • HY-103145
    PNU-22394 hydrochloride
    Agonist 98.79%
    PNU-22394 hydrochloride is an agonist for 5-HT, with Ki of 6.1 and 10 nM, for 5-HT2C and 5-HT2A, respectively.
    PNU-22394 hydrochloride
  • HY-17038S2
    Agomelatine-d3
    Antagonist ≥98.0%
    Agomelatine-d3 is the deuterium labeled Agomelatine. Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
    Agomelatine-d<sub>3</sub>
  • HY-B2089
    Cinitapride
    Modulator 98.24%
    Cinitapride is a nonselective 5-HT1 and 5-HT4 receptors agonist and a 5-HT2 and D2 antagonist. Cinitapride can be used in functional dyspepsia (FD) and gastroesophageal reflux disease (GERD) research.
    Cinitapride
  • HY-U00286
    5-HT2A antagonist 1
    Antagonist
    5-HT2A antagonist 1 is a 5-HT2A antagonist extracted from patent US5728835A and JP 1007727. 5-HT2A antagonist 1 may be useful in treatment of gastrointestinal disorders circulatory disorders.
    5-HT2A antagonist 1
  • HY-103108
    CJ033466
    Agonist 98.29%
    CJ033466 is a novel and selective 5-HT4 receptor partial agonist with an EC50 of 9 nM and has gastroprokinetic effect.
    CJ033466
  • HY-116795
    5-Methoxy-α-ethyltryptamine
    98.91%
    5-Methoxy-α-ethyltryptamine is a tryptamine psychoactive substance, which has nerve stimulated effect.
    5-Methoxy-α-ethyltryptamine
  • HY-105090
    Lerisetron
    Antagonist 99.18%
    Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats.
    Lerisetron
  • HY-B0002BS
    Ondansetron-d5
    Antagonist ≥99.0%
    Ondansetron-d5 is the deuterium labeled Ondansetron. Ondansetron (GR 38032; SN 307) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy.
    Ondansetron-d<sub>5</sub>
  • HY-A0021C
    (R,R)-Palonosetron Hydrochloride
    99.61%
    (R,R)-Palonosetron Hydrochloride is the active enantiomer of Palonosetron.
    (R,R)-Palonosetron Hydrochloride
  • HY-100166
    AP521
    Agonist 98.96%
    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
    AP521
  • HY-U00373
    Revexepride
    Agonist 99.84%
    Revexepride is a highly selective 5-HT4 receptor agonist, and a potential inducer of CYP3A4 enzyme, used for the treatment of gastroesophageal reflux disease.
    Revexepride
  • HY-103140
    Ro60-0175 fumarate
    Agonist 99.47%
    Ro60-0175 fumarate is a potent and selective agonist of 5-HT2C receptor.
    Ro60-0175 fumarate
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