2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

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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-HT Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-B1473A
    Serotonin
    		Agonist 99.86%
    Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
    Serotonin
  • HY-B1473
    Serotonin hydrochloride
    		Agonist 99.97%
    Serotonin (5-Hydroxytryptamine) hydrochloride is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist, with blood-brain barrier permeability. Serotonin hydrochloride is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
    Serotonin hydrochloride
  • HY-19545A
    SCH-23390 hydrochloride
    		Agonist 99.83%
    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.
    SCH-23390 hydrochloride
  • HY-N0122
    5-Hydroxytryptophan
    		Agonist 99.92%
    5-Hydroxytryptophan, a tryptophan metabolite, is a direct 5-hydroxytryptamine (5-HT) precursor and an L-aromatic amino acid decarboxylase substrate. .
    5-Hydroxytryptophan
  • HY-B0670A
    Dihydroergotamine mesylate
    		Agonist 99.94%
    Dihydroergotamine mesylate is a BBB-permeable ergot alkaloid that can be used for the research of migraines.
    Dihydroergotamine mesylate
  • HY-14546
    Aripiprazole
    		Agonist 99.95%
    Aripiprazole (OPC-14597), an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole can be used for the research of schizophrenia and COVID19.
    Aripiprazole
  • HY-112061
    8-OH-DPAT
    		Agonist 99.87%
    8-OH-DPAT is a potent, brain-penetrant and selective 5-HT agonist, with a pIC50 of 8.19 for 5-HT1A and a Ki of 466 nM for 5-HT7; 8-OH-DPAT weakly binds to 5-HT1B (pIC50, 5.42), 5-HT (pIC50 <5).
    8-OH-DPAT
  • HY-14262
    Vilazodone
    		Agonist 99.73%
    Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
    Vilazodone
  • HY-103124
    DOI hydrochloride
    		Agonist 99.61%
    DOI hydrochloride is a serotonin 5-HT2A/2C receptor agonist with Ki values of 0.7 nM, 2.4 nM and 20 nM for h5-HT2A, h5-HT2C and h5-HT2B receptors, respectively. DOI hydrochloride can across the blood-brain barrier. DOI hydrochloride increases head twitches in mice.
    DOI hydrochloride
  • HY-B2132
    Tryptamine
    		Agonist 99.89%
    Tryptamine is a selective, blood-brain-penetrating 5-HT4 receptor agonist (EC50=1-3 mM) and an endogenous ligand of the aryl hydrocarbon receptor (AHR) (Kd=10-50 nM). Tryptamine promotes intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs) and accelerates gastrointestinal motility. Tryptamine regulates Th17/Treg balance to inhibit neuroinflammation, competitively binds to 5-HT receptors to regulate central nervous system activity, and participates in temperature regulation and spinal reflex regulation as a neuromodulator. Tryptamine can be used to study intestinal motility disorders such as functional constipation, and has shown significant efficacy in multiple sclerosis models.
    Tryptamine
  • HY-101369
    BW-723C86
    		Agonist 99.74%
    BW-723C86 is an orally active and a selective 5-HT2B receptor agonist. BW-723C86 exhibits anxiolytic-like actions. BW-723C86 also causes hyperphagia and reduced grooming in rats. BW-723C86 dilates pulmonary arteries and inhibits liquid meal-induced gastric accommodation.
    BW-723C86
  • HY-B1115A
    Buspirone
    		Agonist 99.86%
    Buspirone is an orally active 5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research.
    Buspirone
  • HY-14151
    Prucalopride
    		Agonist 99.93%
    Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.
    Prucalopride
  • HY-14149
    Cisapride
    		Agonist 99.87%
    Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity.
    Cisapride
  • HY-14544
    Quetiapine
    		Agonist 99.93%
    Quetiapine (ICI204636) is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
    Quetiapine
  • HY-14261
    Vilazodone Hydrochloride
    		Agonist 99.94%
    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
    Vilazodone Hydrochloride
  • HY-14153A
    Tegaserod maleate
    		Agonist 99.90%
    Tegaserod maleate (SDZ-HTF-919) is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod maleate has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod maleate causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod maleate has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
    Tegaserod maleate
  • HY-B1473AS
    Serotonin-d4
    		Agonist 99.61%
    Serotonin-d4 is deuterium labeled Serotonin. Serotonin is a monoamine neurotransmitter in the CNS and an endogenous 5-HT receptor agonist. Serotonin is also a catechol O-methyltransferase (COMT) inhibitor with a Ki of 44 μM.
    Serotonin-d<sub>4</sub>
  • HY-75502
    Rotigotine
    		Agonist 99.98%
    Rotigotine is a potent dopamine receptor agonist with Ki values of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors and dopamine D1 receptor. Rotigotine a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor. Rotigotine can be used for parkinson's disease (PD) research.
    Rotigotine
  • HY-B0121B
    Sumatriptan
    		Agonist 99.96%
    Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research.
    Sumatriptan
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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