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-14539A
    Clozapine hydrochloride
    Modulator 99.83%
    Clozapine hydrochloride (HF 1854 hydrochloride) is an antipsychotic used for the research of schizophrenia. Clozapine hydrochloride has high affinity for a number of neuroreceptors. Clozapine hydrochloride is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine hydrochloride inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine hydrochloride is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
    Clozapine hydrochloride
  • HY-100656AS
    Desmethyl cariprazine-d8
    99.90%
    Desmethyl cariprazine-d8 is the deuterium labeled Desmethyl cariprazine (HY-100656). Desmethyl cariprazine is a major active metabolite of cariprazine, with activities at human dopamine receptors and serotonin receptors, showing a pEC50 of 8.90 at human D2 receptors, a pEC50 of 8.09 at D3 receptors, and a pEC50 of 6.28 at 5-HT1A receptors. Desmethyl cariprazine inhibits forskolin-induced cAMP production at D2, D3 and 5-HT1A receptors, and suppresses serotonin-induced Ca2+ release at 5-HT2B receptors. Desmethyl cariprazine is applicable to research related to schizophrenia, bipolar disorder type I and bipolar disorder.
    Desmethyl cariprazine-d<sub>8</sub>
  • HY-100658S
    Didesmethyl cariprazine-d8
    99.40%
    Didesmethyl cariprazine-d8 is the deuterium labeled Didesmethyl cariprazine (HY-100658). Didesmethyl cariprazine is an orally active, BBB-permeable metabolite of Cariprazine (HY-14763). Didesmethyl cariprazine is a partial agonist at the D2 and D3 receptors, full agonist at the 5-HT1A receptor, and antagonist at the human 5-HT2B receptor (Ki: 1.41 nM (human D2L), 0.056 nM (human D3), 1.7 nM (human 5-HT1A), 0.52 nM (human 5-HT2B)). Didesmethyl cariprazine dose-dependently inhibits the spontaneous activity of rat midbrain dopaminergic neurons.
    Didesmethyl cariprazine-d<sub>8</sub>
  • HY-N0737AR
    Harmine (Standard)
    Inhibitor
    Harmine (Standard) is the analytical standard of Harmine. This product is intended for research and analytical applications. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
    Harmine (Standard)
  • HY-126057A
    (S)-Praziquantel
    Control 99.35%
    S)-Praziquantel is a inactive distomer of R-praziquantel.
    (S)-Praziquantel
  • HY-N0737AG
    Harmine (GMP)
    Inhibitor
    Harmine (GMP) (Telepathine (GMP)) is Harmine (HY-N0737A) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
    Harmine (GMP)
  • HY-162677
    MT-1207
    Antagonist 99.96%
    MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research.
    MT-1207
  • HY-116076
    S-15535
    Modulator 99.82%
    S-15535 is a highly selective 5-HT1A receptor ligand. S-15535 is an antagonist of postsynaptic 5-HT1A receptors and an agonist of presynaptic 5-HT1A receptors. S-15535 can be used in research on psychiatric disorders, such as anti-anxiety.
    S-15535
  • HY-101924
    AVN-492
    Antagonist 99.30%
    AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
    AVN-492
  • HY-109167
    Aramisulpride
    Antagonist 98.49%
    Aramisulpride (R-(+)-Amisulpride) is the R-isomer of Amisulpride (HY-14545). Aramisulpride is a 5-HT7 receptor antagonist with a Ki value of 22 nM. Aramisulpride is a D2/D3 receptor antagonist with a Ki value of 140 nM for D2R and a Ki value of 13.9 nM for D3R. Aramisulpride can be used in psychiatric research.
    Aramisulpride
  • HY-B0965AS
    Thioridazine-d3 hydrochloride
    Antagonist 98.25%
    Thioridazine-d3 (hydrochloride) is the deuterium labeled Thioridazine. 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-d<sub>3</sub> hydrochloride
  • HY-B1517AR
    Alprenolol hydrochloride (Standard)
    Antagonist
    Alprenolol (hydrochloride) (Standard) is the analytical standard of Alprenolol (hydrochloride). This product is intended for research and analytical applications. 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 (Standard)
  • HY-14546A
    Aripiprazole monohydrate
    Agonist 99.83%
    Aripiprazole (OPC-14597) monohydrate, an atypical antipsychotic, is a potent and high-affinity dopamine D2 receptor partial agonist. Aripiprazole monohydrate is an inverse agonist at 5-HT2B and 5-HT2A receptors and displays partial agonist actions at 5-HT1A, 5-HT2C, D3, and D4 receptors. Aripiprazole monohydrate can be used for the research of schizophrenia and COVID19.
    Aripiprazole monohydrate
  • HY-14348
    GSK163090
    Antagonist 99.57%
    GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4, 8.5 and 9.7, respectively. GSK163090 inhibits the functional activity of serotonin reuptake transporter (SerT) with a pKi value of 6.1. GSK163090 has antidepressant and anxiolytic activities.
    GSK163090
  • HY-103133
    WAY208466 dihydrochloride
    Agonist 98.43%
    WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex. WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects.
    WAY208466 dihydrochloride
  • HY-19950
    5-HT2A receptor agonist-6
    Agonist 99.79%
    5-HT2A receptor agonist-6 (compound 47) is a selective 5-HT2A receptor agonist (pEC50=6.58).
    5-HT2A receptor agonist-6
  • HY-110094
    BIMU 8
    Agonist 99.60%
    BIMU 8 is a potent and selective 5-HT4 agonist with EC50s of 18 nM, 77 nM, and 540 nM for wild type 5HT4 receptor, T3.36A, and W6.48A mutant 5-HT4 receptors.
    BIMU 8
  • HY-145463
    α-Methylserotonin
    Agonist
    α-Methylserotonin is a potent and selective agonist of 5-HT2 receptor. α-Methylserotonin is an analogue of serotonin formed in vivo from α-methyltryptophan. α-Methylserotonin mediates the lymphatic smooth muscle contraction and prevents the up-regulation of serotonin-receptor-mediated phosphoinositide hydrolysis.
    α-Methylserotonin
  • HY-W100249
    MMAI
    Activator 99.08%
    MMAI is a selective serotonin releaser that can be used in the research of mental illnesses.
    MMAI
  • HY-W009754
    Antidepressant agent 10
    Inhibitor 99.96%
    Antidepressant agent 10 (Compound 4) is an orally active compound. Antidepressant agent 10 has IC50 values of 190 nM and 110 nM for 5-HT1A and 5-HT2, respectively. Antidepressant agent 10 can be used in the research of mental disorders.
    Antidepressant agent 10
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