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-P1422
    Spadin
    Inducer 99.08%
    Spadin, a natural peptide derived from a propeptide released in blood, is a potent TREK-1 channel blocker with IC50 value of 10 nM. Spadin enhances dorsal raphe nucleus 5-HT neurotransmission in mice and induces hippocampal CREB activation and neurogenesis. Spadin can be used for antidepressant research.
    Spadin
  • HY-W052508
    Norquetiapine
    Modulator 99.95%
    Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats.
    Norquetiapine
  • HY-B0198A
    Cefaclor monohydrate
    99.11%
    Cefaclor is a well-absorbed orally active cephalosporin antibiotic. Cefaclor can specifically bind to specific for penicillin-binding protein 3 (PBP3). Cefaclor can be used for the research of depression and kinds of infections caused by bacteria, such as respiratory tract infections, bacterial bronchitis, pharyngitis and skin infections.
    Cefaclor monohydrate
  • HY-W010869
    GR 55562 hydrochloride
    Antagonist
    GR 55562 hydrochloride is a selective 5-HT1B receptor antagonist. GR 55562 hydrochloride can be used for the research of nerve disease.
    GR 55562 hydrochloride
  • HY-B1541
    Bemesetron
    Antagonist ≥99.0%
    Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM. Neuroprotective effect.
    Bemesetron
  • HY-101248
    GR-46611
    Agonist 99.82%
    GR-46611 is a 5-HT1D receptor agonist. GR-46611 can be used in the research of bladder hyperactivity, leukemia.
    GR-46611
  • HY-120738
    p-MPPI hydrochloride
    Antagonist 99.81%
    p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with high affinity for 5-HT1A receptors. p-MPPI hydrochloride can crosses the blood-brain barrier, and has clear antidepressant and anxiolytic-like effects.
    p-MPPI hydrochloride
  • 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-103118
    PU02
    Antagonist ≥99.0%
    PU02, a derivative of 6-MP (HY-13677), is a negative allosteric modulator (NAM) of 5-HT3 receptor, with IC50 values of 0.36 and 0.73 μM in HEK293 cells transfected with human 5-HT3A and 5-HT3AB receptors respectively.
    PU02
  • HY-101698B
    Alniditan dihydrochloride
    Agonist 99.70%
    Alniditan (Alnitidan) dihydrochloride is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK?293 cells, respectively. Alniditan dihydrochloride has migraine-preventive effects.
    Alniditan dihydrochloride
  • HY-14546S
    Aripiprazole-d8
    Agonist ≥99.0%
    Aripiprazole-d8 is the deuterium labeled Aripiprazole, which is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
    Aripiprazole-d<sub>8</sub>
  • HY-100330
    YM348
    Agonist 99.15%
    YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
    YM348
  • HY-14431
    Cerlapirdine
    Antagonist 98.84%
    Cerlapirdine (SAM-531, PF-05212365) is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. Cerlapirdine has the potential for researching the Alzheimer's disease.
    Cerlapirdine
  • HY-14147
    Renzapride
    Agonist 98.36%
    Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study.
    Renzapride
  • HY-110289
    (R)-Citalopram oxalate
    Inhibitor 99.52%
    (R)-Citalopram oxalate is an anticonvulsant, antidepressant and muscle relaxant. (R)-Citalopram oxalate is at least 20-fold weaker than S-citalopram (Escitalopram; HY-14258) as inhibitor of the 5-HT transporter (SERT). (R)-Citalopram oxalate functionally antagonises S-citalopram in vivo and in vitro. (R)-Citalopram oxalate has an effect on the association of Escitalopram with the high affinity primary site, and on its dissociation from the 5-HT transporter, via an allosteric mechanism.
    (R)-Citalopram oxalate
  • HY-B0061
    Tandospirone citrate
    Agonist 99.79%
    Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
    Tandospirone citrate
  • HY-B0115A
    Pizotifen malate
    Antagonist 99.88%
    Pizotifen malate (Pizotyline malate) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.
    Pizotifen malate
  • 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-110033
    Ecopipam hydrobromide
    Antagonist ≥99.0%
    Ecopipam (SCH 39166) hydrobromide is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrobromide can be used for the research of schizophrenia and obesity.
    Ecopipam hydrobromide
  • HY-116565A
    Usmarapride free base
    Agonist 99.91%
    Usmarapride (SUVN-D4010) free base is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) free base can be used for the research of cognitive deficits associated with Alzheimer's disease.
    Usmarapride free base
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