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-100851A
    LY-272015 hydrochloride
    		Antagonist 99.54%
    LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats.
    LY-272015 hydrochloride
  • HY-118166
    Gentisein
    		Inhibitor 98.13%
    Gentisein (NSC 329491), the major metabolite of Mangiferin, shows the most potent serotonin uptake inhibition with an IC50 value of 4.7 µM.
    Gentisein
  • HY-B0740
    Cyclobenzaprine hydrochloride
    		Antagonist 99.59%
    Cyclobenzaprine (MK130) hydrochloride is an orally active 5-HT2 receptor antagonist. Cyclobenzaprine hydrochloride acts centrally, providing skeletal muscle relaxation, alleviating muscle spasms, and reducing pain. Additionally, Cyclobenzaprine hydrochloride has antiprotozoal activity. Additionally, Cyclobenzaprine hydrochloride also possesses antiparasitic activity. Cyclobenzaprine hydrochloride holds promise for research in the fields of acute, painful skeletal muscle disorders and infectious diseases
    Cyclobenzaprine hydrochloride
  • HY-101222
    SB-203186 hydrochloride
    		Antagonist 99.94%
    SB-203186 hydrochloride is a potent, selective and competitive 5-HT4 antagonist. SB-203186 hydrochloride antagonizes the 5-HT4 receptor-mediated relaxations of the carbachol-contracted rat isolated oesophagus against 5-HT with pKB values of 10.9 (rat oesophagus), 9.5 (guinea-pig ileum), and 9.0 (human colon) respectively.
    SB-203186 hydrochloride
  • HY-103099
    SB-399885 hydrochloride
    		Antagonist 98.33%
    SB-399885 hydrochloride is a 5-HT6 receptor antagonist.
    SB-399885 hydrochloride
  • HY-117083
    Clothiapine
    		Antagonist 99.93%
    Clothiapine, an atypical antipsychotic agent, shares with clozapine its strong antiserotonergic properties.
    Clothiapine
  • HY-17382A
    Metoclopramide hydrochloride hydrate
    		Antagonist 99.96%
    Metoclopramide hydrochloride hydrate is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide hydrochloride hydrate can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.
    Metoclopramide hydrochloride hydrate
  • HY-B0229
    Zolmitriptan
    		Agonist 99.98%
    Zolmitriptan (BW-311C90; 311C90) is a 5-HT1B/1D receptor partial agonist with Kis of 5.01 nM, 0.63 nM, and 63.09 nM for 5-HT1B, 5-HT1D, 5-HT1F receptor, respectively. Zolmitriptan can be used for the research of migraine.
    Zolmitriptan
  • HY-15472
    PRX-08066
    		Antagonist
    PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.
    PRX-08066
  • HY-14785
    Befiradol
    		Agonist 99.20%
    Befiradol (NLX-112) is a selective 5-HT1A receptor agonist.
    Befiradol
  • HY-14340
    WAY-181187
    		Agonist 98.07%
    WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
    WAY-181187
  • HY-121392
    GR 125743
    		Antagonist 99.77%
    GR 125743 is a selective 5-HT1B/1D receptor antagonist, with pKis of 8.85 and 8.31 for wild-type h5-HT1B and wild-type h5-HT1D, respectively. GR 125743 is used for the research of Parkinson's disease and cardiovascular diseases.
    GR 125743
  • HY-108256
    Melitracen hydrochloride
    		Inhibitor 99.90%
    Melitracen hydrochloride is an orally active biphasic antidepressant and antianxiety agent. Melitracen hydrochloride can inhibit the uptake of Norepinephrine and 5-HT (serotonin) through the presynaptic membrane inducing the increase of monoamine transmitters in synaptic space.
    Melitracen hydrochloride
  • HY-133111
    3-Hydroxy agomelatine
    		Antagonist 98.00%
    3-Hydroxy agomelatine is a metabolite of Agomelatine. 3-Hydroxy agomelatine is a 5-HT2C receptor antagonist with an IC50 of 3.2 μM and a Ki of 1.8 μM.
    3-Hydroxy agomelatine
  • HY-109118A
    Masupirdine mesylate
    		Antagonist 99.62%
    Masupirdine mesylate (SUVN-502 mesylate) is a potent, selective, orally bioavailable, and brain penetrant 5-HT6 receptor antagonist (Ki of 2.04 nM for human 5-HT6 receptor). Masupirdine mesylate (SUVN-502 mesylate) shows high selectivity over 5-HT2A receptor and other 100 target sites, and has potential for treatment of Alzheimer's disease.
    Masupirdine mesylate
  • HY-153912
    5-HT2A receptor agonist-3
    		Agonist 98.53%
    5-HT2A receptor agonist-3 is the most selective agonist for the human 5-HT2A receptor yet discovered, with a Ki of 2.5 nM, and with 124-fold selectivity for 5-HT2A over the structurally similar 5-HT2C receptor.
    5-HT2A receptor agonist-3
  • HY-17038A
    Agomelatine hydrochloride
    		Antagonist 99.98%
    Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
    Agomelatine hydrochloride
  • HY-121301
    Amperozide
    		Antagonist 98.75%
    Amperozide is an atypical antipsychotic that acts as an antagonist of the 5-HT2 receptor with a Ki value of 26 nM. Amperozide has a low affinity for D2 receptors.
    Amperozide
  • HY-12706
    Spiroxatrine
    		Antagonist 99.18%
    Spiroxatrine (R 5188) is a selective, dual antagonist of 5-HT1α and α2-adrenergic, with the Ki values of 3.94, 224000, 118.5 nM for 5-HT1α, 5-HT1β and 5-HT2, respectively. Spiroxatrine (R 5188) has a sedative effect.
    Spiroxatrine
  • HY-14539R
    Clozapine (Standard)
    		Modulator 99.98%
    Clozapine (Standard) is the analytical standard of Clozapine. This product is intended for research and analytical applications. Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
    Clozapine (Standard)
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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