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-105285R
    Piromelatine (Standard)
    Modulator
    Piromelatine (Standard) is the analytical standard of Piromelatine. This product is intended for research and analytical applications. Piromelatine (Neu-P11) is a melatonin MT1/MT2 receptor agonist, serotonin 5-HT1A/5-HT1D agonist, and serotonin 5-HT2B antagonist. Piromelatine (Neu-P11) possesses sleep promoting, analgesic, anti-neurodegenerative, anxiolytic and antidepressant potentials. Piromelatine (Neu-P11) also possesses pain-related P2X3, TRPV1, and Nav1.7 channel-inhibition capacities.
    Piromelatine (Standard)
  • HY-101331A
    Phenylbiguanide hydrochloride
    Agonist
    Phenylbiguanide hydrochloride is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
    Phenylbiguanide hydrochloride
  • HY-103107R
    LY334370 (Standard)
    Agonist
    LY334370 (Standard) is the analytical standard of LY334370. This product is intended for research and analytical applications. LY334370 is a selective 5-HT1F receptor agonist with a Ki of 1.6 nM.
    LY334370 (Standard)
  • HY-164011
    Alaproclate
    Inhibitor
    Alaproclate is an inhibitor for serotonin (5-HT) reuptake. Alaproclate affects mechanisms that related to cued navigation performance such as sensory, sensorimotor, or motivational factors, impairs spatial navigation ability of rats.
    Alaproclate
  • HY-W728110
    5-MeO-pyr-T
    Agonist
    5-MeO-pyr-T (5-Methoxy pyrrolidinyltryptamine) is a 5-HT1AR agonist, with Kis of 0.577 and 373 μM for 5-HT1AR and 5-HT2AR respectively. 5-MeO-pyr-T inhibits 5-HT uptake and elicits 5-HT release. 5-MeO-pyr-T induces hypolocomotion.
    5-MeO-pyr-T
  • HY-101309A
    5-(Nonyloxy)tryptamine oxalate
    Agonist
    5-(Nonyloxy)tryptamine oxalate, a high-affinity agonist for the 5-HTIDβ receptor, with an ED50 value of 68 nM. 5-(Nonyloxy)tryptamine oxalate, exhibits antitumor growth activity in vivo and enhances the ability of T cells to target tumor cells.
    5-(Nonyloxy)tryptamine oxalate
  • HY-108057
    Facinicline
    Antagonist
    Facinicline (RG3487) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM.
    Facinicline
  • HY-123480
    EGIS-7625
    Inhibitor
    EGIS-7625 is a selective and competitive 5-HT2B inhibitor with pKi values of 9.0, 6.2, 7.7 for 5-HT2B, 5-HT2A, 5-HT2C, respective. EGIS-7625 partially attenuates m-chlorophenylpiperazine-induced hypomotility and hypophagia.
    EGIS-7625
  • HY-105082
    Avitriptan
    Agonist
    Avitriptan is a 5-HT1B/1D receptor agonist, with pKis of 7.44 ( 5-HT1B rat), 7.68 ( 5-HT1B human) and 8.36 ( 5-HT1D human). Avitriptan constricts the isolated coronary artery. Avitriptan can be used for migraines.
    Avitriptan
  • HY-107626
    ATC0065
    ATC0065 is a potent, selective and orally active melanin-concentrating hormone (MCH) receptor 1 (MCHR1) antagonist with an IC50 of 15.7 nM for human MCHR1. ATC0065 does not exhibits significant activity for MCHR2. ATC0065 has anxiolytic and antidepressant activities.
    ATC0065
  • HY-119389
    RGH-1756
    Antagonist
    RGH-1756 is an atypical antipsychotic that has a strong and selective antagonist activity on human D3 and less pronounced activity on human D2L and 5HT1A receptors.
    RGH-1756
  • HY-109065
    Minesapride
    Agonist
    Minesapride is a partial agonist with a highly selective serotonin 4 (5-HT4) receptor. Minesapride enhances gastrointestinal peristalsis and colon transport by activating the 5-HT4 receptor. Minesapride increases bowel movements and suppresses visceral allergic reactions. Minesapride can be used in the study of constipation-type irritable bowel syndrome (IBS-C).
    Minesapride
  • HY-B0602C
    Desvenlafaxine hydrochloride
    Inhibitor
    Desvenlafaxine (O-Desmethylvenlafaxine) hydrochloride is a selective serotonin and norepinephrine reuptake inhibitor. Desvenlafaxine (O-Desmethylvenlafaxine) hydrochloride is the major metabolite of the antidepressant venlafaxine. Desvenlafaxine (O-Desmethylvenlafaxine) hydrochloride has the potential for the research of depression and related disorders and diseases (extracted from patent WO2009049354A1).
    Desvenlafaxine hydrochloride
  • HY-14338
    Idalopirdine
    Antagonist
    Idalopirdine (Lu AE58054 ) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.
    Idalopirdine
  • HY-101630A
    Deramciclane fumarate
    Antagonist
    Deramciclane fumarate is an antagonist of 5-HT Receptor. Deramciclane fumarate is an inverse agonist of 5-HT2C Receptor with an IC50 of 168 nM. Deramciclane fumarate also decreases basal phosphoinositide hydrolysis.
    Deramciclane fumarate
  • HY-B1396S3
    Nefazodone-d4 hydrochloride
    Antagonist
    Nefazodone-d4 (hydrochloride) (BMY-13754-d4) is deuterium labeled Nefazodone (hydrochloride). Nefazodone hydrochloride (BMY-13754) is a potent and selective 5HT2A (Ki=5.8 nM) antagonist with moderate inhibition of 5-HT and noradrenaline uptake (IC50 of 290 and 300 nM, respectively). Nefazodone hydrochloride is a phenylpiperazine antidepressant with less alpha-adrenergic blocking activity.
    Nefazodone-d<sub>4</sub> hydrochloride
  • HY-B0197S
    Naratriptan-d3
    Agonist
    Naratriptan-d3 (GR-85548A-d3) is the deuterium labeled Naratriptan (HY-B0197). Naratriptan is a selective 5-HT1B/1D receptor agonist. Naratriptan is peripherally active and has good oral bioavailability, inducing cranial artery vasoconstriction by activating 5-HT1B/1D receptors (EC50=0.11 μM for dog basilar artery). Naratriptan also inhibits trigeminal nerve-mediated dural neurogenic plasma extravasation and reduces sterile inflammation. Naratriptan is mainly used in the research of acute migraine, targeting cranial vascular and neuroinflammatory mechanisms.
    Naratriptan-d<sub>3</sub>
  • HY-32329S
    Setiptiline-d3
    Modulator
    Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine[1][2].
    Setiptiline-d<sub>3</sub>
  • HY-Z6430
    Des-4-fluorobenzyl mosapride
    Agonist
    Des-4-fluorobenzyl mosapride is the primary metabolite of Mosapride (HY-B0189). Mosapride is an orally active gastroenterokinetic compound and is a 5HT4 agonist.
    Des-4-fluorobenzyl mosapride
  • HY-169457
    Aeruginascin
    Agonist
    Aeruginascin is an indole derivative and a tryptamine that can be extracted from Inocybe aeruginascens Babos . Aeruginascin may cause an euphoric mood during psychosis with hallucinations.
    Aeruginascin
Cat. No. Product Name / Synonyms Application Reactivity