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-17410
    Iloperidone
    Antagonist 99.93%
    Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.
    Iloperidone
  • HY-B0750
    Dolasetron
    Antagonist ≥98.0%
    Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
    Dolasetron
  • HY-B0072
    Tropisetron
    Antagonist 99.93%
    Tropisetron is an orally active 5-HT3R antagonist (Ki = 5.3 nM) as well as being a potent and selective α7 nicotinic partial agonist (EC50 = 1.3 μM). Tropisetron prevents phosphorylation and activation of the p38 MAPK. Tropisetron inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibits the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is anti-inflammatory and antiemetic. Tropisetron has antitumor and neuroprotective effects. Tropisetron can be studied in research for diseases including hemorrhagic cystitis, chronic joint inflammation, lung cancer and chronic cerebral hypoperfusion.
    Tropisetron
  • HY-103151
    CP94253 hydrochloride
    Agonist 98.84%
    CP94253 hydrochloride is a potent and selective agonist of 5-HT1B receptor (Ki= 2 nM in a radioligand binding assay).Ki values for 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors are 89, 49, 860, and 1600 nM respectively. CP94253 hydrochloride is centrally active upon systemic administration in vivo.
    CP94253 hydrochloride
  • HY-A0095A
    Flibanserin hydrochloride (propan-2-ol) hydrate
    Modulator 99.04%
    Flibanserin (BIMT-17) hydrochloride (propan-2-ol) hydrate is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin hydrochloride (propan-2-ol) hydrate binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin hydrochloride (propan-2-ol) hydrate shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research-.
    Flibanserin hydrochloride (propan-2-ol) hydrate
  • HY-149170
    FFN246
    99.79%
    FFN246 is a fluorescent, dual substrate of serotonin transporter (SERT) probe and vesicular monoamine transporter 2 (VMAT2) with excitation and emission spectra 392/427 nm. FFN246 can be used for labeling serotonergic neurons in mouse brain tissue through SERT-dependent accumulation.
    FFN246
  • HY-100665
    Dehydroaripiprazole
    Agonist 99.94%
    Dehydroaripiprazole (OPC-14857) is an active metabolite of Aripiprazole (HY-14546) and dopamine D2/D3 receptor partial agonist. Dehydroaripiprazole also has certain affinity for serotonin 5-HT1A, 5-HT2A and 5-HT2B receptors. Dehydroaripiprazole has antipsychotic activity equivalent to Aripiprazole.
    Dehydroaripiprazole
  • HY-19733
    Lumateperone tosylate
    Antagonist 99.78%
    Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
    Lumateperone tosylate
  • HY-U00096
    Ansofaxine hydrochloride
    Inhibitor 99.72%
    Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.
    Ansofaxine hydrochloride
  • HY-B0965A
    Thioridazine
    Antagonist 99.50%
    Thioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
    Thioridazine
  • HY-19863
    F-15599
    Agonist 99.13%
    F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
    F-15599
  • HY-B0020
    Tropisetron Hydrochloride
    Antagonist 99.97%
    Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation.
    Tropisetron Hydrochloride
  • HY-123630
    Allura Red AC
    Activator 98.01%
    Allura Red AC is a food colorant, appearing as a deep red water-soluble powder or granules, used in various applications such as beverages, syrups, candies, and cereals. Allura Red AC can statically quench the intrinsic fluorescence of HSA. Additionally, Allura Red AC is a 5-hydroxytryptamine (5-HT) pathway-associated pro-inflammatory agent, capable of exacerbating experimental colitis. Allura Red AC holds potential for research in inflammatory bowel disease (IBD), intestinal barrier function, and food additive safety.
    Allura Red AC
  • HY-19889
    JNJ-18038683
    Antagonist 99.76%
    JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
    JNJ-18038683
  • HY-103137
    Zacopride hydrochloride
    99.69%
    Zacopride hydrochloride is an orally active 5-HT3 receptor (Ki of 0.38 nM) antagonist and 5-HT4 receptor (Ki of 373 nM) agonist. Zacopride hydrochloride exhibits multiple activities, such as regulating gastrointestinal motility, affecting cardiac function, and exerting anxiolytic and antiemetic effects. Zacopride hydrochloride is currently mainly used in the research of gastrointestinal diseases, cardiovascular diseases, and psychiatric diseases such as anxiety.
    Zacopride hydrochloride
  • HY-111200
    Vabicaserin hydrochloride
    Agonist 99.47%
    Vabicaserin hydrochloride is a 5-hydroxytryptamine 2C (5-HT2C) receptor-selective agonist with an EC50 of 8 nM.
    Vabicaserin hydrochloride
  • HY-B0068
    Azasetron hydrochloride
    Antagonist 99.76%
    Azasetron (Y-25130) hydrochloride, a benzamide derivative, is a potent and selective 5-HT3 receptor antagonist. Azasetron is used in the study for Chemotherapy-induced nausea and vomiting (CINV).
    Azasetron hydrochloride
  • HY-103093
    Zotepine
    Antagonist 99.85%
    Zotepine, an antipsychotic agent, is a potent antagonist of 5-HT2A, 5-HT2C, Histamine H1, α1-adrenergic and Dopamine D2 receptors, with Kds of 2.6 nM, 3.2 nM, 3.3 nM, 7.3 nM and 8 nM, respectively. Zotepine exhibits antidepressive and anxiolytic effects in vivo.
    Zotepine
  • HY-B0002
    Ondansetron hydrochloride
    Antagonist 99.94%
    Ondansetron (GR 38032; SN 307) hydrochloride is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride can inhibit nausea and vomiting induced by chemotherapy and radiotherapy.
    Ondansetron hydrochloride
  • HY-20696
    Tetrahydro-β-carboline
    Inhibitor 99.40%
    Tetrahydro-β-carboline (Tryptoline) is a metabolite of tryptamine, also is a competitive serotonin reuptake inhibitor with an Ki value of 6.1 µM.
    Tetrahydro-β-carboline
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