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-139233
    25P-NBOMe hydrochloride
    		Agonist
    25P-NBOMe hydrochloride is structurally categorized as a phenethylamine. 25P-NBOMe hydrochloride binds 5-HT receptors 5-HT2A and 5-HT2C with similar affinities.
    25P-NBOMe hydrochloride
  • HY-105699
    Napamezole
    		Inhibitor
    Napamezole is an orally active α-2 adrenergic receptor antagonist and serotonin (5-HT Receptor) reuptake inhibitor, with Ki values of 28 nM and 93 nM for rat α-2 and α-1 adrenergic receptors, respectively. Napamezole can be used for the research of depression.
    Napamezole
  • HY-10564S1
    Sarpogrelate-d4 hydrochloride
    		Antagonist
    Sarpogrelate-d4 (MCI-9042-d4) hydrochloride is deuterium labeled Sarpogrelate (hydrochloride). Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
    Sarpogrelate-d<sub>4</sub> hydrochloride
  • HY-182091
    CYD-1-79
    		Agonist
    CYD-1-79 is a selective positive allosteric modulator of 5-HT2C receptor. CYD-1-79 potentiates 5-HT-evoked intracellular calcium release via a topographically distinct allosteric site. CYD-1-79 shows significant inhibition of binding at dopamine D3 receptor, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 modulates 5-HT2C receptor-mediated spontaneous ambulation in rodents and synergizes with a low dose of a 5-HT2C receptor agonist. CYD-1-79 attenuates relapse vulnerability of psychoactive substance in a rodent self-administration model. CYD-1-79 can be used for the research of neurological disease.
    CYD-1-79
  • HY-129682
    LY125180
    		Inhibitor
    LY125180 is a serotonin uptake inhibitor. LY125180 competitively inhibits the uptake of serotonin and norepinephrine by cortical synaptosomes and of dopamine by striatal synaptosomes, with Ki values of 0.06 μM, 2.2 μM and 2.5 μM respectively.
    LY125180
  • HY-180617
    5-HT2CR allosteric modulator 1
    		Agonist
    5-HT2CR modulator 1 (Compound 3B) is a selective, positive ago-allosteric modulator of 5HT2CR with an EC50 of 8 nM. 5-HT2CR modulator 1 is also a selective 5HT2CR agonist with an EC50 of 25 nM. 5-HT2CR modulator 1 reduces food intake.
    5-HT2CR allosteric modulator 1
  • HY-172978
    5-HT2A receptor agonist-8
    		Agonist
    5-HT2A receptor agonist-8 (compound 8) is a potent 5-HT2A receptor agonist with an EC50 of 0.6784 nM. 5-HT2A receptor agonist-8 can be used in the study of depressive disorders and bipolar disorders.
    5-HT2A receptor agonist-8
  • HY-19733S
    Lumateperone-CHC,d3 tosylate
    		Antagonist
    Lumateperone-13C,d3 (ITI-007-13C,d3) tosylate is 13C and deuterium labeled Lumateperone (tosylate). Lumateperone (ITI-007) tosylate is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a dopamine D1 receptor modulator. Lumateperone tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
    Lumateperone-</sup>CH<sub>C,d<sub>3</sub> tosylate
  • HY-100703S
    Pipamperone-d10 dihydrochloride
    		Antagonist
    Pipamperone-d10 (Floropipamide-d10) dihydrochloride is a deuterated Pipamperone dihydrochloride (HY-100703A). Pipamperone dihydrochloride (Floropipamide dihydrochloride) is a butyrophenone derivative and high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0). Pipamperone dihydrochloride is also a low-affinity antagonist of D2 receptor (pKi=6.7). Pipamperone dihydrochloride affects neurotransmitter functions and exerts antipsychotic activity. Pipamperone dihydrochloride is used in the research of mental disorders such as autism-related behavioral disorders and Alzheimer's disease.
    Pipamperone-d<sub>10</sub> dihydrochloride
  • HY-133112
    7-Desmethyl-3-hydroxyagomelatine
    		Antagonist
    7-Desmethyl-3-hydroxyagomelatine (3-Hydroxy-7-desmethyl agomelatine), a metabolite of Agomelatine, has less activity than Agomelatine. Agomelatine is a melatonergic (MT1 and MT2) agonist and serotonergic (5HT2C) antagonist.
    7-Desmethyl-3-hydroxyagomelatine
  • HY-143329
    MAO-B-IN-3
    MAO-B-IN-3 is a reversible and selective MAO-B inhibitor (IC50=96 nM). MAO-B-IN-3 also binds to 5-HT6R with Ki value of 696 nM. MAO-B-IN-3 can be used for research of in Alzheimer's disease.
    MAO-B-IN-3
  • HY-171194
    VU0530244
    		Antagonist
    VU0530244 is a potent antagonist of 5-HT2B, with the IC50 of 17.3 nM. VU0530244 is predicted to have very limited potential for brain penetration in human subjects, as is predicted to be substrates for P-gp-mediated efflux in humans.
    VU0530244
  • HY-117046
    AVN-101
    		Antagonist
    AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
    AVN-101
  • HY-136109H
    (Rac)-Ulotaront hydrochloride
    		Agonist
    (Rac)-Ulotaront hydrochloride ((Rac)-SEP-363856 hydrochloride) is the racemate of Ulotaront hydrochloride (HY-136109). Ulotaront hydrochloride, an orally active and CNS active psychotropic agent with a unique, non-D2/5-HT2A mechanism of action, exerts its antipsychotic-like effects. Ulotaront has the potential for the treatment of schizophrenia.
    (Rac)-Ulotaront hydrochloride
  • HY-W751350
    Cyclobenzaprine-d6
    		Antagonist
    Cyclobenzaprine-d6 is the deuterium labeled Cyclobenzaprine. 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. 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-d<sub>6</sub>
  • HY-B0366AR
    Cyproheptadine hydrochloride (Standard)
    		Antagonist
    Cyproheptadine (hydrochloride) (Standard) is the analytical standard of Cyproheptadine (hydrochloride). This product is intended for research and analytical applications. Cyproheptadine hydrochloride is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine hydrochloride has antiplatelet and thromboprotective activities. Cyproheptadine hydrochloride can be used for the research of thromboembolic disorders.
    Cyproheptadine hydrochloride (Standard)
  • HY-14148
    Renzapride hydrochloride
    Renzapride hydrochloride is a benzamide that inhibits irritable bowel syndrome and has antagonistic activity at 5-HT(3) receptors and agonistic activity at 5-HT(4) receptors. Renzapride hydrochloride also exhibits antagonistic activity at 5-HT(2B) receptors and has a certain affinity for 5-HT(2A) and 5-HT(2C) receptors.
    Renzapride hydrochloride
  • HY-W653969
    Arotinolol-d5 hydrochloride
    		Antagonist
    Arotinolol-d5 (hydrochloride) is deuterium labeled Arotinolol. Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.
    Arotinolol-d<sub>5</sub> hydrochloride
  • HY-103114
    AT1015 hydrochloride
    		Antagonist
    AT1015 hydrochloride is a potent antagonist of 5-HT2 receptor, with the pKi of 7.94. AT1015 inhibits vasoconstriction and blocks platelet aggregation.
    AT1015 hydrochloride
  • HY-123829
    LY2624803
    		Inhibitor
    LY2624803 is a 5-HT2A and histamine, H1 receptor antagonist.
    LY2624803
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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