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-59201A
    A-582941 dihydrochloride
    Agonist 99.78%
    A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.
    A-582941 dihydrochloride
  • HY-16688A
    RU 24969 succinate
    Agonist 99.58%
    RU 24969 succinate is a 5-HT receptor agonist with Ki values of 0.38 and 2.5 nM for 5-HT1B and 5-HT1A, respectively. RU 24969 decreases fluid consumption and increases forward locomotion. RU 24969 succinate can be used for the research of neurological disease.
    RU 24969 succinate
  • HY-101357A
    CP 93129 dihydrochloride
    Agonist ≥99.0%
    CP 93129 dihydrochloride is a potent 5HT1B receptor agonist. CP 93129 dihydrochloride has the potential for parkinson's disease research.
    CP 93129 dihydrochloride
  • HY-B0383A
    Almotriptan
    Agonist 99.94%
    Almotriptan is a selective agonist of 5-HT 1B/1D Receptor. Almotriptan can used in study of migraine attacks.
    Almotriptan
  • HY-103129
    SB-200646A
    Antagonist 99.89%
    SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
    SB-200646A
  • HY-124821
    VA012
    Modulator 99.34%
    VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin 5-HT2C receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research.
    VA012
  • HY-W050162
    (E)-3,4,5-Trimethoxycinnamic acid
    Inhibitor 99.95%
    (E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.
    (E)-3,4,5-Trimethoxycinnamic acid
  • HY-103415
    Nemonapride
    Agonist 99.90%
    Nemonapride is a highly potent dopamine D2 receptor antagonist with a Ki of 0.06 nM. Nemonapride also activates 5-HT1A receptor with an IC50 of 34 nM. Nemonapride is an antipsychotic that readily passes through the blood brain barrier and exhibits potent neuroleptic effects in animals.
    Nemonapride
  • HY-100552
    VUF10166
    Antagonist 99.83%
    VUF10166 is a potent and high-affinity 5-HT3 receptor antagonist, with Ki values of 0.04 nM (5-HT3A) and 22 nM (5-HT3AB). VUF10166 inhibits 5-HT-induced responses at 5-HT3A and 5-HT3AB receptors at nanomolar concentrations. At 5-HT3 receptor, VUF10166 at higher concentrations also acts as a partial agonist, with an EC50 of 5.2 μM.
    VUF10166
  • HY-103136
    R-96544
    Antagonist 99.50%
    R-96544 is an orally active 5-HT2A receptor antagonist. R-96544 can inhibit platelet aggregation in vitro.
    R-96544
  • HY-W795507
    Cyanopindolol
    Antagonist 99.24%
    Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively).
    Cyanopindolol
  • HY-110023
    Zimelidine dihydrochloride
    Inhibitor 98.27%
    Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine dihydrochloride is an antidepressant.
    Zimelidine dihydrochloride
  • HY-120083
    Rodatristat
    Inhibitor 98.41%
    Rodatristat (KAR5417) is a potent tryptophan hydroxylase 1 (TPH1) and TPH2 inhibitor with IC50s value of 33 nM and 7 nM, respectively, and shows robust reduction of intestinal serotonin (5-HT) levels in mice.
    Rodatristat
  • HY-14541S
    Olanzapine-d3
    Antagonist 99.09%
    Olanzapine-d3 is the deuterium labeled Olanzapine. Olanzapine is a selective, orally active monoaminergic antagonist with high affinity binding to serotonin H1, 5HT2A/2C, 5HT3, 5HT6 (Ki=7, 4, 11, 57, and 5 nM, respectively), dopamine D1-4 (Ki=11 to 31 nM), muscarinic M1-5 (Ki=1.9-25 nM), and adrenergic α1 receptors (Ki=19 nM). Olanzapine is an atypical antipsychotic.
    Olanzapine-d<sub>3</sub>
  • HY-10559
    Nelotanserin
    Antagonist 99.52%
    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
    Nelotanserin
  • HY-111419
    DSP-1053
    Agonist 99.75%
    DSP-1053, a benzylpiperidine derivative, is a potent Serotonin Transporter (SERT) inhibitor with a Ki of 1.02 nM. DSP-1053 shows partial 5-HT1A receptor agonistic activity with a Ki of 5.05 nM. DSP-1053 has antidepressant activity.
    DSP-1053
  • HY-167902
    YM-31636 free base
    Agonist 99.05%
    YM-31636 free base is an orally active, potent and selective 5-HT3 receptor agonist with a Ki value of 0.2 nM. YM-31636 free base induces contraction of isolated guinea pig distal colon. YM-31636 free base induces tachycardia with the relative intrinsic activity of approximately 0.23 in isolated guinea pig right atrium. YM-31636 free base is promising for research of constipation.
    YM-31636 free base
  • HY-19650
    Pumosetrag Hydrochloride
    Agonist 99.77%
    Pumosetrag Hydrochloride (MKC-733; DDP-733) is an orally available 5-HT3 partial agonist developed for the treatment of irritable bowel syndrome and gastroesophageal reflux disease.
    Pumosetrag Hydrochloride
  • 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-B0031S1
    Quetiapine-d4 hemifumarate
    Agonist 99.69%
    Quetiapine-d4 (hemifumarate) is the deuterium labeled Quetiapine hemifumarate. Quetiapine hemifumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects.
    Quetiapine-d<sub>4</sub> hemifumarate
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