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

5-HT 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.

5-HT Receptor Related Products (615):

Cat. No. Product Name Effect Purity
  • HY-136109
    SEP-363856 hydrochloride Agonist 99.57%
    SEP-363856 hydrochloride (SEP-856 hydrochloride), an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. SEP-363856 hydrochloride (SEP-856 hydrochloride) has the potential for the study of schizophrenia[1].
  • HY-14940
    Volinanserin Antagonist 99.76%
    Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
  • HY-11018
    Risperidone Inhibitor 98.01%
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-19545A
    SCH-23390 hydrochloride Agonist 99.91%
    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[1][2][3].
  • HY-14539
    Clozapine Modulator 99.99%
    Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].
  • HY-118836
    GSK215083 Antagonist
    GSK215083 is a high affinity 5-HT6 receptor antagonist. GSK215083 can serves as a promising 5-HT6 radioligand candidate by radiolabeled with (11)C via methylation[1].
  • HY-123704
    CGS-12066 maleate Agonist
    CGS-12066 (maleate) is a 5-HT receptor agonist. CGS-12066 has agonist effect for 5-HT1A , 5-HT1B ,5-HT1C and 5-HT1D with pEC50 values of 6.41, 7.56, 4.05 and 7.11, respectively. CGS-12066 can be used for the research of neurological disease[1].
  • HY-143329
    MAO-B-IN-3
    MAO-B-IN-3 is a reversible and selective MAO-B inhibitor (IC50=96 nM). MAO-B-IN-3 also binds to 5-HT6R with Ki value of 696 nM. MAO-B-IN-3 can be used for research of in Alzheimer's disease[1].
  • HY-14153AS
    Tegaserod-13C,d3 maleate Modulator
    Tegaserod-13C,d3 (maleate) is the 13C- and deuterium labeled Tegaserod (maleate). Tegaserod maleate is a selective 5-HT4 receptor partial agonist and a 5-HT2B receptor antagonist. Tegaserod maleate exhibits a promotile effect throughout the gastrointestinal (GI) tract[1][2][5].
  • HY-103113
    MS 245 oxalate Antagonist
    MS 245 oxalate is a potent antagonist of 5-HT6 receptor with a Ki of 2 nM[1].
  • HY-U00443
    SB 258719 Antagonist
    SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease[1][2][3].
  • HY-B0031S
    Quetiapine-d4 fumarate Agonist
    Quetiapine-d4 (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects[1].
  • HY-16688B
    RU 24969 hemisuccinate Agonist
    RU 24969 hemisuccinate 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 hemisuccinate could decrease fluid consumption and increase forward locomotion[1].
  • HY-B0071
    Granisetron Antagonist
    Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
  • HY-14763S
    Cariprazine-d6 Modulator 98.00%
    Cariprazine-d6 is a deuterium labeled Cariprazine. Cariprazine Cariprazine is an antipsychotic agent that exhibits high affinity for the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM)[1].
  • HY-16567
    Asenapine hydrochloride Antagonist 98.76%
    Asenapine hydrochloride, an antipsychotic, is a 5-HT (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) and Dopamine (D2, D3, D4) receptor antagonist with Ki values of 0.03-4.0 nM for 5-HT and 1.3, 0.42, 1.1 nM for Dopamine receptor, respectively.
  • HY-111455
    LP-211 Agonist 99.61%
    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).
  • HY-N3398
    Lauroscholtzine Agonist
    Lauroscholtzine (N-Methyllaurotetanine), a natural alkaloid, is a 5-HT1A receptor agonist[1].
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride Inhibitor 99.65%
    Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
  • HY-W011235S
    Norfluoxetine-d5 hydrochloride 99.57%
    Norfluoxetine-d5 (hydrochloride) is deuterium labeled 3-Phenyl-3-(4-(trifluoromethyl)phenoxy)propan-1-amine hydrochloride.