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-A0007
    Rotigotine Hydrochloride
    Agonist 99.45%
    Rotigotine Hydrochloride (N-0923 Hydrochloride) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Ki 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 Hydrochloride
  • HY-B1115
    Buspirone hydrochloride
    Agonist 99.99%
    Buspirone hydrochloride is a 5-HT1A receptor agonist. Buspirone hydrochloride can be used for anxiety and depression research.
    Buspirone hydrochloride
  • HY-156601
    Bexicaserin
    Agonist 99.83%
    Bexicaserin (LP352) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related disorders (such as epilepsy).
    Bexicaserin
  • HY-14153
    Tegaserod
    Agonist 99.71%
    Tegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
    Tegaserod
  • HY-15688
    8-OH-DPAT hydrobromide
    Agonist 99.88%
    8-OH-DPAT (8-Hydroxy-DPAT) hydrobromide is a potent, brain-penetrant and selective 5-HT1A agonist with a pIC50 of 8.19. 8-OH-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.
    8-OH-DPAT hydrobromide
  • HY-172420
    Bretisilocin
    Agonist 99.69%
    Bretisilocin (GM-2505) is the agonist for 5-HT2A receptor and a serotonin releaser. Bretisilocin exhibits antidepressant activity and can be used in the study of depression.
    Bretisilocin
  • HY-100554
    BMY 7378
    Agonist 99.92%
    BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist.
    BMY 7378
  • HY-19358
    2-Methyl-5-HT
    Agonist 98.93%
    2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT is shown to display anti-depressive-like effects.
    2-Methyl-5-HT
  • HY-111455
    LP-211
    Agonist 99.87%
    LP-211 is a selective and blood brain barrier penetrant 5-HT7 receptor agonist, with a Ki of 0.58 nM, with high selectivity over 5-HT1A receptor (Ki, 188 nM) and D2 receptor (Ki, 142 nM).
    LP-211
  • HY-102064
    SR 57227A
    Agonist 99.86%
    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.
    SR 57227A
  • HY-B0031
    Quetiapine hemifumarate
    Agonist 99.96%
    Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate 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 hemifumarate
  • HY-101341
    RS 67333 hydrochloride
    Agonist 99.68%
    RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.
    RS 67333 hydrochloride
  • HY-12694
    Prucalopride succinate
    Agonist 99.94%
    Prucalopride succinate 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 succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.
    Prucalopride succinate
  • HY-100938
    m-CPBG hydrochloride
    Agonist 99.85%
    m-CPBG (1-(3-Chlorophenyl)biguanide) hydrochloride is a selective 5-HT3 agonist. m-CPBG hydrochloride can be used for the research of neurological disease.
    m-CPBG hydrochloride
  • HY-16688
    RU 24969
    Agonist 99.77%
    RU 24969 is a preferential 5-HT1B agonist, with a Ki of 0.38 nM, but also displays appreciable affinity for the 5-HT1A receptor (Ki=2.5 nM), and has low affinity for other receptor sites in the brain. RU 24969 could decrease fluid consumption and increase forward locomotion.
    RU 24969
  • HY-B0121
    Sumatriptan succinate
    Agonist 99.89%
    Sumatriptan succinate (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 succinate can be used for migraine headache research.
    Sumatriptan succinate
  • HY-W015169
    5-Methoxytryptamine
    Agonist 99.91%
    5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action.
    5-Methoxytryptamine
  • HY-B0206
    Rizatriptan benzoate
    Agonist 99.93%
    Rizatriptan benzoate is the agonist for 5-HT1B and 5-HT1D. Rizatriptan benzoate has a peripheral vasoconstrictive effect, penetrates the intact blood-brain barrier, and inhibits pain neurotransmission in the central nervous system.
    Rizatriptan benzoate
  • HY-136109
    Ulotaront hydrochloride
    Agonist 99.89%
    SEP-363856 (SEP-856) hydrochloride, an orally active TAAR1 and 5-HT1A agonist and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride has the potential for the study of schizophrenia.
    Ulotaront hydrochloride
  • HY-B0189A
    Mosapride citrate
    Agonist 99.96%
    Mosapride citrate is an orally active gastroenterokinetic compound. Mosapride citrate is a 5HT4 agonist. Mosapride citrate is a CYP inducer. Mosapride citrate has a concentration-dependent inhibitory effect on Kv4.3, and its IC50 value is 15.2 μM. Mosapride citrate can be used in the study of gastrointestinal diseases.
    Mosapride citrate
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