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-155116
    5-HT6 agonist 1
    Agonist
    5-HT6 agonist 1 (Compound 19) is a 5-HT6 agonist (Ki: 5 nM). 5-HT6 agonist 1 has antidepressant-like properties, and improves cognitive deficits. 5-HT6 agonist 1 also inhibits platelet aggregation. 5-HT6 agonist 1 has high metabolic stability.
    5-HT6 agonist 1
  • HY-15472A
    PRX-08066 maleate
    Antagonist
    PRX-08066 is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR, IC50= 3.4 nM) antagonist that causes selective vasodilation of pulmonary arteries.
    PRX-08066 maleate
  • HY-111491
    Methiothepin
    Antagonist
    Methiothepin (Metitepine; Ro 8-6837) is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
    Methiothepin
  • HY-169446
    ALEPH hydrochloride
    Agonist
    ALEPH (hydrochloride) is the h5-HT2A and h5-HT2B partial agonist with the EC50 values of 10.3 nM and 19.2 nM, respectively. ALEPH (hydrochloride) causes head twitch response in mice (ED50: 0.80 mg/kg).
    ALEPH hydrochloride
  • HY-103146
    GR125487 sulfamate
    Antagonist
    GR125487 sulfamate is an orally active and selective antagonist of 5-HT4R. GR125487 sulfamate effectively blocks the cognition enhancing effect. GR125487 sulfamate can be used to study memory disorders, gastrointestinal disorders, mood disorders and urinary tract dysfunction.
    GR125487 sulfamate
  • HY-101105
    SB-224289
    Antagonist
    SB-224289 is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
    SB-224289
  • HY-107125A
    AVN-322 free base
    Antagonist
    AVN-322 free base is an orally active, highly selective 5-HT6Rantagonist for central nervous system disease research.
    AVN-322 free base
  • HY-118836
    GSK215083
    Antagonist
    GSK215083 is a high affinity 5-HT6 receptor antagonist. GSK215083 can serves as a promising 5-HT6 radioligand candidate by radiolabeled with (11)C via methylation.
    GSK215083
  • HY-153027
    Methylergometrine
    Agonist
    Methylergometrine (Methylergonovine) is an orally active 5-HT2B ligand agonist. The distribution half-life of Methylergometrine is only 1-2 min. Methylergometrine can be used as an oxytocin to treat uterine atony.
    Methylergometrine
  • HY-10351
    Robalzotan
    Inhibitor
    Robalzotan (NAD-​299) is a potent and selective 5-Hydroxytryptamine 1A (5-HT1A) inhibitor. Robalzotan increases the firing rate of 5-HT cells. Robalzotan induces 5-HT1A receptor occupancy. Robalzotan has the potential for the research of a cholinergic deficit in the central -nervous system.
    Robalzotan
  • HY-167663A
    (S)-Ebalzotan
    Agonist
    (S)-Ebalzotan is the S-form of Ebalzotan (HY-167663). Ebalzotan is a 5-HT1A receptor agonist with activity in the study of depression. Ebalzotan can serve as a precursor to important active pharmaceutical ingredients. The synthesis of Ebalzotan involves a multi-enzyme catalyzed reduction reaction to obtain saturated primary or secondary alcohols in high yields and high enantioselectivity.
    (S)-Ebalzotan
  • HY-107626A
    ATC0065 free base
    ATC0065 free base 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 free base does not exhibits significant activity for MCHR2. ATC0065 free base has anxiolytic and antidepressant activities.
    ATC0065 free base
  • HY-107847
    2-(2-Methoxyphenoxy)ethylamine hydrochloride
    Agonist ≥98.0%
    2-(2-Methoxyphenoxy)ethylamine hydrochloride (Compound 2b) is a mixed agonist/antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride is a5-HT1A receptor partial agonist and a α1-adrenergic receptor antagonist. 2-(2-Methoxyphenoxy)ethylamine hydrochloride can be used for neurological diseases research, such as anxiety, depression and psychosis.
    2-(2-Methoxyphenoxy)ethylamine hydrochloride
  • HY-106487
    Pridefine
    Inhibitor
    Pridefine (AHR-1118) is an antidepressant agent.
    Pridefine
  • HY-169791
    ECPLA
    Agonist
    ECPLA, a lysergamide lysergic acid diethylamidean (LSD) analog, is a potent 5-HT2A agonist (EC50 of 14.6 nM) for Gq-mediated calcium flux. ECPLA has high affinity for most serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors.
    ECPLA
  • HY-103139
    Altanserin hydrochloride
    Ligand
    Altanserin is a 5-hydroxytryptamine (5-HT2A ) selective radioligand. Altanserin delivers human serotonin. Altanserin can be used to study the biochemical and cellular mechanisms of vulnerability to extracellular 5-HT increase .
    Altanserin hydrochloride
  • HY-A0095S
    Flibanserin-d4
    Modulator
    Flibanserin-d4 is a deuterium labeled Flibanserin (BIMT-17). Flibanserin is a full agonist of the serotonin 5-HT1A receptor (Ki=1 nM) and an antagonist of 5-HT2A (49 nM).
    Flibanserin-d<sub>4</sub>
  • HY-19417
    Wf-516 hydrochloride
    Antagonist
    Wf-516 hydrochloride is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively.Wf-516 hydrochloride has potent antidepressant activity.
    Wf-516 hydrochloride
  • HY-B0002BS1
    Ondansetron-d3
    Ondansetron-d3 is the deuterium labeled Ondansetron (HY-B0002B ). Ondansetron (GR 38032; SN 307) is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron can inhibit nausea and vomiting induced by chemotherapy and radiotherapy.
    Ondansetron-d<sub>3</sub>
  • HY-124412
    Paynantheine
    Agonist
    Paynantheine is an alkaloid with antinociceptive activity, which is found in Mitragyna speciosa. Paynantheine is also a 5-HT1AR and 5-HT2BR agonist that induces lower lip retraction and antinociception in rats.
    Paynantheine
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