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

5-HT 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:

  • 5-HT1 Receptor

  • 5-HT2 Receptor

  • 5-HT3 Receptor

  • 5-HT5 Receptor

  • 5-HT6 Receptor

  • 5-HT7 Receptor

  • 5-HT Receptor

  • 5-HT4 Receptor

5-HT Receptor Related Products (393):

Cat. No. Product Name Effect Purity
  • HY-19545A
    SCH-23390 hydrochloride Agonist 99.31%
    SCH-23390 hydrochloride (R-(+)-SCH-23390 hydrochloride) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. SCH-23390 hydrochloride is a potent and high efficacy human 5-HT2C receptor agonist with a Ki of 9.3 nM. SCH-23390 hydrochloride also binds with high affinity to the 5-HT2 and 5-HT1C receptors. SCH-23390 hydrochloride inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with an IC50 of 268 nM.
  • HY-N0145
    Puerarin Antagonist 99.20%
    Puerarin, an isoflavone extracted from Radix puerariae, is a 5-HT2C receptor antagonist.
  • HY-14564A
    GTS-21 dihydrochloride Antagonist 99.78%
    GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
  • HY-B0965
    Thioridazine hydrochloride Antagonist 99.93%
    Thioridazine hydrochloride, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine hydrochloride is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine hydrochloride shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
  • HY-15370A
    SB-269970 hydrochloride Antagonist 98.77%
    SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pKi of 8.3, exhibits >50-fold selectivity against other receptors.
  • HY-110129
    Eplivanserin hemifumarate Antagonist
    Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
  • HY-141422A
    4,4-Diphenylbutylamine hydrochloride Antagonist 99.00%
    4,4-Diphenylbutylamine shows affinity for the 5-HT2A and H1 receptors with Kis of 2589 and 1670 nM, respectively.
  • HY-128901
    F13714 fumarate Agonist 98.65%
    F13714 fumarate, a selective 5-HT1A receptor biased agonist, shows antidepressant-like properties after a single administration in the mouse model of chronic mild stress.
  • HY-11018
    Risperidone Inhibitor 98.01%
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-10349A
    WAY-100635 Maleate Inhibitor ≥98.0%
    WAY-100635 maleate is a potent and selective 5-hydroxytryptamine 1A (5-HT1A) receptor antagonist with an IC50 value of 0.91 nM and Ki value of 0.39 nM. WAY-100635 maleate has pIC50 values for 5-HT1A and α1-adrenergic receptors of 8.9 and 6.6, respectively. WAY-100635 maleate is also a potent dopamine D4 receptor agonist.
  • HY-B0670A
    Dihydroergotamine mesylate Agonist 99.91%
    Dihydroergotamine mesylate is an ergot alkaloid used to treat migraines.
  • HY-14546
    Aripiprazole Agonist 99.93%
    Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  • HY-B0527A
    Amitriptyline hydrochloride Inhibitor 99.56%
    Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity.
  • HY-10562
    Ketanserin Antagonist ≥98.0%
    Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
  • HY-B0478
    Trazodone hydrochloride Antagonist 99.87%
    Trazodone (hydrochloride) (AF-1161) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
  • HY-14557
    Pimavanserin Inhibitor 99.78%
    Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
  • HY-B1115
    Buspirone hydrochloride Agonist 99.92%
    Buspirone hydrochloride is an anxiolytic psychotropic drug, is used to treat generalized anxiety disorder (GAD).
  • HY-B0982
    Pindolol Modulator 99.91%
    Pindolol (LB-46) is a nonselective β-blocker with partial beta-adrenergic receptor agonist activity, also functions as a 5-HT1A receptor weak partial antagonist (Ki=33nM).
  • HY-107836
    Methiothepin mesylate Antagonist ≥98.0%
    Methiothepin mesylate is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
  • HY-14149
    Cisapride Agonist 99.72%
    Cisapride(R 51619) is a nonselective 5-HT4 receptor agonist, it is also a potent hERG potassium channel inhibitor.
Isoform Specific Products

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