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-101632
    Irindalone
    Antagonist
    Irindalone is a novel serotonin 5-HT2 antagonist.
    Irindalone
  • HY-19684
    Pancopride
    Antagonist
    Pancopride is a new potent and selective 5-HT3 receptor antagonist.
    Pancopride
  • HY-101668
    Sulamserod
    Antagonist
    Sulamserod is a 5-HT4 receptor antagonist, with antiarrhythmic activities.
    Sulamserod
  • HY-101698
    Alniditan
    Agonist
    Alniditan (Alnitidan) is a potent 5-HT1B and 5-HT1D receptors agonist, with IC50s of 1.7 nM and 1.3 nM for h5-HT1B and h5-HT1D receptors in HEK293 cells, respectively. Alniditan has migraine-preventive effects.
    Alniditan
  • HY-19110
    RG-12915
    Antagonist
    RG-12915 is a selective 5-HT3 antagonist, with IC50 value of 0.16 nM.
    RG-12915
  • HY-101641
    NRA-0160
    NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
    NRA-0160
  • HY-19417A
    Wf-516
    Antagonist
    Wf-516 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, and has potent antidepressant activity.
    Wf-516
  • HY-U00028
    T 82
    Antagonist
    T 82 is a potent 5-HT3 antagonist and acetylcholinesterase (AChE) inhibitor, used for treatment of Alzheimer's Disease.
    T 82
  • HY-14335A
    Ro 04-6790 di(hydrochloride)
    Antagonist
    Ro 04-6790 dihydrochloride is a potent, competitive and selective 5-HT6 receptor antagonist with pKi values of 7.26, 7.35 for rat and human 5-HT6 receptors, respectively. Ro 04-6790 dihydrochloride has no affinity at other receptors.
    Ro 04-6790 di(hydrochloride)
  • HY-B0121BS3
    Sumatriptan-d6 formate
    Agonist
    Sumatriptan-d6 (formate) (GR 43175 free base-d6 (formate)) is deuterium labeled Sumatriptan. Sumatriptan (GR 43175) is an orally active 5-HT1 receptor agonist with IC50s of 7.3 nm, 9.3nm and 17.8 nm for 5-HT1D, 5-HT1B and 5-HT1F receptors, respectively. Sumatriptan can be used for migraine headache research.
    Sumatriptan-d<sub>6</sub> formate
  • HY-19927A
    DA-6886 monohydrochloride
    Agonist
    DA-6886 is a 5-Hydroxytryptamine receptor 4 (5-HT4) agonist. DA-6886 induces relaxation of the rat oesophagus preparation in a 5-HT4 receptor antagonist-sensitive manner. The evaluation of DA-6886 in CHO cells expressing hERG channels reveals that it inhibits hERG channel current with an pIC50 value of 4.3, indicating that the compound is 1000-fold more selective for the 5-HT4 receptor over hERG channels. DA-6886 can be used in the study of constipated irritable bowel syndrome.
    DA-6886 monohydrochloride
  • HY-14261R
    Vilazodone (Hydrochloride) (Standard)
    Agonist
    Vilazodone (Hydrochloride) (Standard) is the analytical standard of Vilazodone (Hydrochloride). This product is intended for research and analytical applications. Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
    Vilazodone (Hydrochloride) (Standard)
  • HY-139045
    2,4-DMA hydrochloride
    Agonist
    2,4-DMA hydrochloride is an amphetamine and is a serotonin 5-HT2 receptor agonist with an apparent PA2 value of 5.6.
    2,4-DMA hydrochloride
  • HY-A0077S2
    Perphenazine-d6 fumarate
    Antagonist
    Perphenazine-d6 (fumarate) is a deuterated labeled Perphenazine. Perphenazine is an orally active dopamine receptor and histamine-1 receptor antagonist, with Ki values of 0.56 nM (D2), 0.43 nM (D3), 6 nM (5-HT2A), respectively. Perphenazine also binds to Alpha-1A adrenergic receptor. Perphenazine inhibits cancer cell proliferation, and induces apoptosis. Perphenazine can be used in the research of mental disease, cancer, inflammation.
    Perphenazine-d<sub>6</sub> fumarate
  • HY-17637S2
    Lumateperone-d4
    Lumateperone-d4 (ITI-007-d4) is deuterium labeled Lumateperone. Lumateperone (ITI-007) is an orally active 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 has anticancer activity and can also be used for the study of schizophrenia and bipolar depression.
    Lumateperone-d<sub>4</sub>
  • HY-118575
    DR-4004
    Antagonist
    DR-4004 is a 5-HT7 receptor antagonist that attenuates the decreased level of performance produced by mCPP and the performance levels after p-chloroamphetamine (PCA) lesion of the 5-HT system. DR-4004 also reverses amnesia induced by Scopolamine (HY-N0296) and Dizocilpine (HY-15084B). DR-4004 is promising for research of schizophrenia, cognitive deficits and atypical antipsychotic agents.
    DR-4004
  • HY-170053
    4-Hydroxy MPT
    Agonist
    4-Hydroxy MPT (4-OH-MPT), a serotonergic hallucinogen, is a 5-HT2A and 5-HT2B receptors agonist with EC50 values of 3.82 nM and 3.4 nM, respectively.
    4-Hydroxy MPT
  • HY-109112R
    Brilaroxazine (Standard)
    Modulator
    Brilaroxazine (Standard) is the analytical standard of Brilaroxazine. This product is intended for research and analytical applications. Brilaroxazine (RP5603) is a potent and orally active multimodal dopamine (DA)/serotonin (5-HT) modulator. Brilaroxazine is a partial agonist of dopamine (DA) D2, D3, and D4 receptors, 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM), and has antagonist activity at 5-HT2B (Ki=0.19 nM), and 5-HT7 (Ki=2.7 nM) receptors. Brilaroxazine is an atypical antipsychotic agent, and has the potential to improve cognitive impairments in neuropsychiatric and neurological diseases in vivo.
    Brilaroxazine (Standard)
  • HY-101668A
    Sulamserod hydrochloride
    Antagonist
    Sulamserod hydrochloride is a 5-HT4 receptor antagonist. Sulamserod hydrochloride can be used in gastrointestinal disease related research.
    Sulamserod hydrochloride
  • HY-14149R
    Cisapride (Standard)
    Agonist
    Cisapride (Standard) is the analytical standard of Cisapride. This product is intended for research and analytical applications. Cisapride (R 51619) is an orally active 5-HT4 receptor agonist with an EC50 value of 140 nM. Cisapride is a hERG blocker with an IC50 value of 9.4 nM. Cisapride is a gastroprokinetic agent that stimulates gastrointestinal motor activity.
    Cisapride (Standard)
Cat. No. Product Name / Synonyms Application Reactivity