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

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

Related Products

PDF 7.25 MB

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-75502
    Rotigotine
    		Agonist 99.99%
    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-107836
    Methiothepin mesylate
    		Antagonist 99.60%
    Methiothepin (Metitepine) 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).
    Methiothepin mesylate
  • HY-11100
    Asenapine maleate
    		Antagonist 99.95%
    Asenapine maleate is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and D2 antagonist with Ki values of 0.03-4.0 nM, 1.3nM, respectively, and an antipsychotic.
    Asenapine maleate
  • 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-103100
    SB-699551
    		Antagonist 99.53%
    SB-699551 is a potent and selective 5-HT5A antagonist with a Ki value of 5.1 μM. SB-699551 increases the phosphorylation levels of CREB and ATF1, and decreases the phosphorylation levels of AKT, PRAS40, P70S6K, FOXO1, and S6RP. SB-699551 improves drug-induced cognitive deficits. SB-699551 improves social withdrawal and forgetfulness. SB-699551 inhibits breast cancer.
    SB-699551
  • HY-A0021
    Palonosetron hydrochloride
    		Antagonist 99.96%
    Palonosetron hydrochloride is a 5-HT3 antagonist primarily used to prevent acute, delayed, and overall chemotherapy-induced nausea and vomiting. In addition, Palonosetron hydrochloride exhibits moderate anti-flavivirus activity and potent anti-Zika virus activity in mammalian cells. Palonosetron hydrochloride also possesses antidepressant activity.
    Palonosetron hydrochloride
  • HY-W019599
    4-Chloro-L-phenylalanine
    		Inhibitor ≥98.0%
    4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2).
    4-Chloro-L-phenylalanine
  • HY-N0096
    Rotundine
    		Antagonist 99.96%
    Rotundine is an antagonist of dopamine D1, D2 and D3 receptors with IC50s of 166 nM, 1.4 μM and 3.3 μM, respectively. Rotundine is also an antagonist of 5-HT1A with an IC50 of 370 nM.
    Rotundine
  • HY-13575
    Blonanserin
    		Antagonist 99.62%
    Blonanserin (AD-5423) is a potent?and orally active 5-HT2A?(Ki=0.812 nM) and?dopamine D2?receptor?(Ki =0.142?nM)?antagonist. Blonanserin is usually acts as an atypical antipsychotic?agent and can be used for the research of extrapyramidal symptoms, excessive?sedation, or?hypotension.
    Blonanserin
  • HY-10564
    Sarpogrelate hydrochloride
    		Antagonist 99.09%
    Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
    Sarpogrelate hydrochloride
  • HY-108324
    (Z)-Thiothixene
    		Antagonist 99.84%
    (Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1.
    (Z)-Thiothixene
  • 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.
    SKF-83566
  • HY-12694
    Prucalopride succinate
    		Agonist 99.95%
    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-B0121
    Sumatriptan succinate
    		Agonist 99.94%
    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-B1517A
    Alprenolol hydrochloride
    		Antagonist 99.76%
    Alprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
    Alprenolol hydrochloride
  • HY-14558
    Tandospirone
    		Agonist 99.41%
    Tandospirone (SM-3997) is a potent and selective 5-HT1A receptor partial agonist, with a Ki of 27 nM. Tandospirone has anxiolytic and antidepressant activities. Tandospirone can be used for the research of the central nervous system disorders and the underlying mechanisms.
    Tandospirone
  • HY-B1396
    Nefazodone hydrochloride
    		Antagonist 99.87%
    Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.
    Nefazodone hydrochloride
  • HY-B1213
    Trimipramine maleate
    		Antagonist 99.82%
    Trimipramine maleate is a 5-HT receptor antagonist, with pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy.
    Trimipramine maleate
  • HY-18099A
    S1RA hydrochloride
    		Antagonist 99.94%
    S1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.
    S1RA hydrochloride
  • HY-P1422A
    Spadin TFA
    		Inducer 99.73%
    Spadin TFA, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with an IC50 value of 10 nM. Spadin TFA enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin TFA can be used for antidepressant research.
    Spadin TFA
Cat. No. Product Name / Synonyms Application Reactivity