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-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-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-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)
  • HY-137111A
    p-MPPF
    Antagonist
    p-MPPF is a selective 5-HT antagonist that dose-dependently antagonizes the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT (HY-112061) in rats. p-MPPF can be used for neurological disease research.
    p-MPPF
  • HY-Z4466
    Olanzapine ketolactam
    Control
    Olanzapine ketolactam (compound 1) is the impurity of Olanzapine (HY-14541). Olanzapine is a selective, orally active monoaminergic antagonist.
    Olanzapine ketolactam
  • HY-101331R
    Phenylbiguanide (Standard)
    Agonist
    Phenylbiguanide (Standard) is the analytical standard of Phenylbiguanide. This product is intended for research and analytical applications. Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
    Phenylbiguanide (Standard)
  • HY-W015169R
    5-Methoxytryptamine (Standard)
    Agonist
    5-Methoxytryptamine (Standard) is the analytical standard of 5-Methoxytryptamine (HY-W015169). This product is intended for research and analytical applications. 5-Methoxytryptamine, a metabolite of Melatonin, is a nonselective 5-HT receptor agonist. 5-Methoxytryptamine has no affinity for the 5-HT3 receptor. 5-Methoxytryptamine is also a potent antioxidant and has radioprotective action.
    5-Methoxytryptamine (Standard)
  • HY-123514
    SNAP8719 free base
    SNAP8719 free base is a selective α1D-adrenoceptor antagonist (pKi = 8.89). SNAP8719 free base shows affinity for the dopamine D2-, 5-HT1A-, and the human clonal α2a-adrenoceptor, with pKi values of 5.98, 6.47, and <5.0, respectively. SNAP8719 free base causes a concentration-dependent increase in the twitch response.
    SNAP8719 free base
  • HY-116581
    5-HT7R antagonist 4
    Antagonist
    5-HT7R antagonist 4 (Compound 4) is a potent 5-HT7 receptor antagonist (Ki=2.6 nM) with low binding affinity for the 5-HT1A receptor (Ki= 476 nM). 5-HT7R antagonist 4 is promising for research of neurological diseases.
    5-HT7R antagonist 4
  • HY-A0008R
    Talipexole dihydrochloride (Standard)
    Antagonist
    Talipexole (dihydrochloride) (Standard) is the analytical standard of Talipexole (dihydrochloride). This product is intended for research and analytical applications. Talipexole dihydrochloride (B-HT 920 dihydrochloride) is a dopamine D2 receptor agonist, α2-adrenoceptor agonist and 5-HT3 receptor antagonist, which displays antiParkinsonian activity.
    Talipexole dihydrochloride (Standard)
  • HY-169440
    6-Fluoro-N,N-diethyltryptamine
    Ligand
    6-Fluoro-N,N-diethyltryptamine (6-F-DET) has affinity for 5-HT2A receptors.
    6-Fluoro-N,N-diethyltryptamine
  • HY-N0737R
    Harmine hydrochloride (Standard)
    Inhibitor
    Harmine Hydrochloride (Telepathine Hydrochloride) is a natural DYRK inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
    Harmine hydrochloride (Standard)
  • HY-100703R
    Pipamperone (Standard)
    Antagonist
    Pipamperone (Standard) is the analytical standard of Pipamperone (HY-100703). This product is intended for research and analytical applications. Pipamperone (Floropipamide) is a butyrophenone derivative and high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0). Pipamperone is also a low-affinity antagonist of D2 receptor (pKi=6.7). Pipamperone affects neurotransmitter functions and exerts antipsychotic activity. Pipamperone is used in the research of mental disorders such as autism-related behavioral disorders and Alzheimer's disease.
    Pipamperone (Standard)
  • HY-101369R
    BW-723C86 (Standard)
    Agonist
    BW-723C86 (Standard) is the analytical standard of BW-723C86 (HY-101369). This product is intended for research and analytical applications. BW-723C86 is an orally active and a selective 5-HT2B receptor agonist. BW-723C86 exhibits anxiolytic-like actions. BW-723C86 also causes hyperphagia and reduced grooming in rats. BW-723C86 dilates pulmonary arteries and inhibits liquid meal-induced gastric accommodation.
    BW-723C86 (Standard)
  • HY-12560C
    (S)-PNU-282987 hydrochloride
    Antagonist
    (S)-PNU-282987 hydrochloride is an isoform of PNU-282987 (HY-12560). PNU-282987 (free base) is a potent α7 nicotinic acetylcholine receptor (nAChR) agonist with an EC50 of 154 nM. PNU-282987 (free base) is also a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. PNU-282987 (free base) can be used for the research of central and peripheral nervous systems.
    (S)-PNU-282987 hydrochloride
  • HY-W708023
    5-APDI hydrochloride
    Inhibitor
    5-APDI hydrochloride is an indane with an amphetamine-like aminopropane group. 5-APDI hydrochloride inhibits the uptake of serotonin, dopamine, and norepinephrine by crude synaptosomes (IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively).
    5-APDI hydrochloride
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