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 (321):

Cat. No. Product Name Effect Purity
  • HY-B0407A
    Chlorpromazine hydrochloride Antagonist 99.90%
    Chlorpromazine Hydrochloride is an antagonist of the dopamine D2, 5HT2A, potassium channel and sodium channel. Chlorpromazine binds with D2 and 5HT2A with Kis of 363 nM and 8.3 nM, respectively.
  • HY-B1473
    Serotonin hydrochloride Agonist 99.97%
    Serotonin hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
  • 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-N0737A
    Harmine Inhibitor 99.93%
    Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
  • HY-14541
    Olanzapine Antagonist 99.89%
    Olanzapine (LY170053) is a selective monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptor (Ki=19 nM). Olanzapine is an atypical antipsychotic.
  • HY-103129
    SB-200646A Antagonist 99.47%
    SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
  • HY-103430A
    SKF-83566 Antagonist 99.86%
    SKF-83566 is a potent, blood-brain permeable and orally active D1-like dopamine receptor (D1DR) antagonist and a weaker competitive antagonist at the vascular 5-HT2 receptor (Ki=11 nM). SKF-83566 is a competitive DAT (dopamine transporter) inhibitor with an IC50 of 5.7 μM. SKF-83566 also shows selective inhibition for adenylyl cyclase 2 (AC2) over AC1 and AC5 in the isolated rabbit thoracic aorta. SKF-83566 can be used for research of parkinson’s disease and nicotine craving alleviation.
  • HY-102064
    SR 57227A Agonist 99.57%
    SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
  • HY-B0965
    Thioridazine hydrochloride Antagonist 99.93%
    Thioridazine hydrochloride is an antipsychotic drug, used in the treatment of schizophrenia and psychosis, shows D4 selectivity or serotonin antagonism.
  • HY-11018
    Risperidone Inhibitor 99.16%
    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-N0145
    Puerarin Antagonist 99.20%
    Puerarin, an isoflavone extracted from Radix puerariae, is a 5-HT2C receptor antagonist.
  • HY-14546
    Aripiprazole Agonist 99.98%
    Aripiprazole (OPC-14597) is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  • HY-14543
    Sertindole Antagonist 99.76%
    Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.
  • HY-10562
    Ketanserin Antagonist 98.57%
    Ketanserin is a selective 5-HT2 receptor antagonist. Ketanserin also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
  • 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-15780
    Brexpiprazole Modulator 99.40%
    Brexpiprazole (OPC-34712), an atypical antipsychotic drug, is 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.
  • 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-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-14557
    Pimavanserin Inhibitor 99.99%
    Pimavanserin is a selective inverse agonist of the 5-HT2A receptor with pIC50 and pKd of 8.73 and 9.3, respectively.
  • HY-B0032A
    Lurasidone Modulator 99.49%
    Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.
Isoform Specific Products

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