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

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

Related Products

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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.

5-HT Receptor Isoform Specific Products:

5-HT Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-110232
    Risperidone-d4
    		Inhibitor 99.40%
    Risperidone-d4 is the deuterium labeled Risperidone. 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.
    Risperidone-d<sub>4</sub>
  • 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-119541
    Ampreloxetine
    		Inhibitor 98.49%
    Ampreloxetine (TD-9855) is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine has the potential for the research of neurogenic orthostatic hypotension.
    Ampreloxetine
  • 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-110129
    Eplivanserin hemifumarate
    		Antagonist 98.07%
    Eplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
    Eplivanserin hemifumarate
  • HY-117575A
    WAY-100135 dihydrochloride
    		Antagonist 98.32%
    WAY-100135 dihydrochloride is a selective antagonist at presynaptic and postsynaptic 5-HT1A receptor, with an IC50 of 34 nM at the rat hippocampal 5-HT1A receptor. WAY-100135 dihydrochloride has potential antipsychotic properties.
    WAY-100135 dihydrochloride
  • HY-156601A
    (S)-Bexicaserin
    		Agonist 99.93%
    (S)-Bexcaserin (compound 2) is a 5-HT2C receptor agonist with potential for studying obesity and psychiatric-related diseases.
    (S)-Bexicaserin
  • HY-103131
    PNU-142633
    		Agonist 98.6%
    PNU-142633 is a high affinity, selective and orally active 5-HT1D receptor agonist with Kis of 6 nM and > 18 000 nM for human 5-HT1D receptor and human 5-HT1B receptor, respectively. PNU-142633 has anti-migraine efficacy.
    PNU-142633
  • 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-133113
    7-Desmethyl-agomelatine
    		Antagonist 99.89%
    7-Desmethyl-agomelatine is a metabolite of Agomelatine. Agomelatineis a potent agonist at melatonin receptors (MT1 and MT2), and also is an antagonist of 5-HT2C.
    7-Desmethyl-agomelatine
  • HY-N4157
    Isopteropodine
    		Agonist 98.66%
    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-10560
    Temanogrel
    		Antagonist 98.14%
    Temanogrel is a highly selective 5-HT2A receptor antagonist with a Ki of 4.9 nM.
    Temanogrel
  • 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>
  • HY-15543A
    CP-809101 hydrochloride
    		Agonist 99.37%
    CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence.
    CP-809101 hydrochloride
  • HY-14264
    Cyamemazine
    		Antagonist 99.42%
    Cyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.
    Cyamemazine
  • HY-B0031R
    Quetiapine (hemifumarate) (Standard)
    		Agonist 99.87%
    Quetiapine (hemifumarate) (Standard) is the analytical standard of Quetiapine (hemifumarate). This product is intended for research and analytical applications. Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
    Quetiapine (hemifumarate) (Standard)
  • HY-B0527AR
    Amitriptyline (hydrochloride) (Standard)
    		Inhibitor 99.03%
    Amitriptyline (hydrochloride) (Standard) is the analytical standard of Amitriptyline (hydrochloride). This product is intended for research and analytical applications. 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 (hydrochloride) (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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