2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

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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-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-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-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-113254
    13,14-Dihydro-15-keto-PGE2
    13,14-Dihydro-15-keto-PGE2 participates in Bifidobacterium animalis F1-7 to alleviate opioid-induced constipation by 5-HT pathway.
    13,14-Dihydro-15-keto-PGE2
  • 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-W795507
    Cyanopindolol
    		Antagonist 98.67%
    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-15370
    SB-269970
    		Antagonist 98.48%
    SB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors.
    SB-269970
  • 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-111419
    DSP-1053
    		Agonist 99.72%
    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-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
  • 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-135096
    Amitriptyline-d3 hydrochloride
    		Inhibitor 99.46%
    Amitriptyline-d3 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.
    Amitriptyline-d3 hydrochloride
  • HY-14348
    GSK163090
    		Antagonist 99.77%
    GSK163090 is a potent, selective and orally active 5-HT1A/1B/1D receptor antagonist with pKi values of 9.4/8.5/9.7, 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-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-156601A
    (S)-Bexicaserin
    		Agonist 99.93%
    (S)-Bexicaserin ((S)-LP352) (Compound 3) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related disorders.
    (S)-Bexicaserin
  • HY-14782
    Adoprazine
    		Agonist 98.60%
    Adoprazine (SLV313) is a full 5-HT1A receptor agonist with a pEC50 of 9 at cloned h5-HT1A receptors. Adoprazine (SLV313) is a full D2 and D3 receptor antagonist with pA2s of 9.3 and 8.9 at hD2 and hD3 receptors, respectively. Adoprazine (SLV313) has the characteristics of atypical antipsychotics.
    Adoprazine
  • HY-N4157
    Isopteropodine
    		Agonist 99.13%
    Isopteropodine is heteroyohimbine-type oxindole alkaloid components of Uncaria tomentosa (Willd.) DC. Isopteropodine acts as positive modulators of muscarinic M1 and 5-HT2 receptors.
    Isopteropodine
  • HY-N1745
    2'-O-Methylisoliquiritigenin
    		Activator 98.44%
    2'-O-Methylisoliquiritigenin, isolated from the Arachis species, up-regulates 5-HT, NE, DA and GABA pathways, but does not put a very significant effect on ne NE pathway.
    2'-O-Methylisoliquiritigenin
  • HY-B0478R
    Trazodone (hydrochloride) (Standard)
    		Antagonist 99.90%
    Trazodone (hydrochloride) (Standard) is the analytical standard of Trazodone (hydrochloride). This product is intended for research and analytical applications. Trazodone (hydrochloride) (AF-1161) is an antidepressant belonging to the class of serotonin receptor antagonists and reuptake inhibitors for treatment of anxiety disorders.
    Trazodone (hydrochloride) (Standard)
  • HY-14763S1
    Cariprazine-d8
    		Modulator 99.51%
    Cariprazine-d8 is a deuterium labeled Cariprazine. Cariprazine is a novel antipsychotic agent candidate that exhibits high affinity for the D3 (Ki=0.085 nM) and D2 (Ki=0.49 nM) receptors, and moderate affinity for the 5-HT1A receptor (Ki=2.6 nM).
    Cariprazine-d<sub>8</sub>
Cat. No. Product Name / Synonyms Application Reactivity