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-175194
    5-HT2C agonist-6
    Agonist
    5-HT2C agonist-6 (Compound 13), a tricyclic psychedelic psychoplastogen, is a 5-HT2C agonist with an EC50 of 13.8  nM. 5-HT2C agonist-6 can be used for neurological diseases research.
    5-HT2C agonist-6
  • HY-167677
    ASP-2205
    Agonist
    ASP-2205 is a 5-HT2C receptor agonist (human 5-HT2C receptor, EC50=0.85 nM; rat 5-HT2C receptor, EC50=2.5 nM). ASP-2205 enhances the pudendal nerve-mediated urethral closure reflex through the 5-HT2C receptor, thereby preventing urinary incontinence.
    ASP-2205
  • HY-120627
    BMS-442606
    Agonist
    BMS-442606, the S-enantiomer of 6-hydroxybuspirone (6OHB), is an orally active 5-HT1A partial agonist. BMS-442606 can be used for generalized anxiety disorder (GAD) research.
    BMS-442606
  • HY-100171A
    PRX933
    Agonist
    PRX933 (BVT-933) is a 5-HT2C agonist that can be used in the study of obesity and glaucoma.
    PRX933
  • HY-169394
    5-HT1AR agonist 2
    Agonist
    5-HT1AR agonist 2 (Compound 4f) is a 5-HT1A receptor agonist (Ki: 10.0 nM). 5-HT1AR agonist 2 also binds to the SERT, D2 receptor and 5-HT6 receptor (Ki: SERT, 2.8 nM; D2, 23 nM; 5-HT6, 192 nM). 5-HT1AR agonist 2 is stabilized in microsomes and induces hypothermia in mice.
    5-HT1AR agonist 2
  • HY-148032
    5-Benzyloxytryptamine
    Agonist
    5-Benzyloxytryptamine (5-BT) is a selective partial agonist for 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors with an IC50 value of 40 nM for bovine caudate 5-HT1D and reduced affinity for other receptors (5-HT2 IC50>470 nM). 5-Benzyloxytryptamine inhibits adenylate cyclase to decrease neurotransmitter release and downregulate cAMP signaling. 5-Benzyloxytryptamine is promising for research of neurotransmitter imbalance-related disorders like migraine.
    5-Benzyloxytryptamine
  • HY-101225
    8 Hydroxy PIPAT oxalate
    Agonist
    8 Hydroxy PIPAT oxalate is a selective 5-HT1A receptor agonist that promotes the release of histamine from enteric mast cells. 8 Hydroxy PIPAT oxalate activates serotonergic signaling pathways, leading to the degranulation of mast cells in both guinea pig and human intestinal preparations. 8 Hydroxy PIPAT oxalate enhances the spontaneous release of histamine, which may contribute to the regulation of gastrointestinal functions. 8 Hydroxy PIPAT oxalate has potential implications for understanding and treating functional gastrointestinal disorders such as irritable bowel syndrome.
    8 Hydroxy PIPAT oxalate
  • HY-15394A
    (Rac)-Rotigotine
    Agonist
    (Rac)-Rotigotine (N-0437) is a racemate of Rotigotine. Rotigotine is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
    (Rac)-Rotigotine
  • HY-14782A
    Adoprazine hydrochloride
    Agonist
    Adoprazine (SLV313) hydrochloride is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine hydrochloride is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine has the characteristics of atypical antipsychotics.
    Adoprazine hydrochloride
  • HY-A0039
    Eletriptan
    Agonist
    Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine.
    Eletriptan
  • HY-171232
    Jimscaline
    Agonist
    Jimscaline (compound R-(-)2) is a 5-HT2A agonist and mescaline analogue that can be utilized in neurological research.
    Jimscaline
  • HY-14152
    Prucalopride hydrochloride
    Agonist
    Prucalopride hydrochloride is an orally active, selective and specific 5-HT4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride hydrochloride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride hydrochloride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride hydrochloride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.
    Prucalopride hydrochloride
  • HY-B1658BS
    Frovatriptan-d3 succinate
    Agonist
    Frovatriptan-d3 (succinate) is deuterium labeled Frovatriptan (succinate). Frovatriptan succinate ((R)-Frovatriptan succinate) is a potent, high affinity, selective and orally active 5-HT1B (pK50 of 8.2) and 5-HT1D receptor agonist. Frovatriptan succinate exhibits >10-fold selectivity for 5-HT1B and 5-HT1D over 5-HT1A, 5-HT1F, and 5-HT7 and >1000-fold selectivity over other 5-HT, dopamine, histamine H1, and α1-adrenoceptor. Frovatriptan succinate has the potential for migraine research.
    Frovatriptan-d<sub>3</sub> succinate
  • HY-165624A
    (S)-LY-41
    Agonist
    (S)-LY-41, R-enantiomer of LY-41 (HY-165624), is 2-Sminotetralin (HY-W022362) derivative and 8-OH-DPAT (HY-112061) analogue. (S)-LY-41 is a potent and selective 5-HT1A receptor agonist. (S)-LY-41 can reduce the accumulation of 5-hydroxytryptophan (the precursor for 5-HT synthesis) in the rat brain induced by decarboxylase inhibitors (NSD 1015). (S)-LY-41 can lower the body temperature of rats and inhibit the escape response from the cage. (S)-LY-41 can induce the 5-HT behavioral syndrome. (S)-LY-41can be used for the research of neurological disease, such as depression and anxiety.
    (S)-LY-41
  • HY-183577
    5-HT2A agonist 10
    Agonist
    5-HT2A agonist 10 is a 5-HT2A receptor agonist with an EC50 of 9 nM. 5-HT2A agonist 10 is applicable to research related to central nervous system diseases.
    5-HT2A agonist 10
  • HY-14262S1
    Vilazodone-d8 hydrochloride
    Agonist
    Vilazodone-d8 hydrochloride is deuterated labeled Vilazodone (HY-14262). 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-d<sub>8</sub> hydrochloride
  • HY-175657
    5-HT2A receptor agonist-12
    Agonist
    5-HT2A receptor agonist-12 (compound 161-2) is a potent 5-HT2A agonist with an EC50 value of <100 nM for h5-HT2A.
    5-HT2A receptor agonist-12
  • HY-127141
    Cizolirtine citrate
    Agonist
    Cizolirtine citrate (E-4018) is an analgesic agent. Cizolirtine citrate has significant analgesic and anti-hyperalgesic action in neuropathic pain models.
    Cizolirtine citrate
  • HY-167893
    AGH-107
    Agonist
    AGH-107 is a high selective and brain-penetrant agonist of 5-HT7 receptor, with a Ki of 6 nM and EC50 of 19 nM. AGH-107 exhibits high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures.
    AGH-107
  • HY-174146
    5-HT1A agonist 1
    Agonist
    5-HT1A agonist 1 (Compound Ex.37) is a highly selective 5-HT1a receptor agonist (EC50=0.18 nM). 5-HT1A agonist 1 mimicks serotonin binding to the receptor, promotes postsynaptic membrane hyperpolarization, inhibits neuronal hyperexcitability, and reduces the release of anxiety-related neurotransmitters. 5-HT1A agonist 1 is promising for research of neuropsychiatric diseases.
    5-HT1A agonist 1
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