2. Signaling Pathways
  3. GPCR/G Protein
    Neuronal Signaling
  4. 5-HT Receptor

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-100923
    H-9 Dihydrochloride
    		Inhibitor 98.98%
    H-9 Dihydrochloride is a PKA (protein kinase) inhibitor. H-9 Dihydrochloride (10 μM) significantly reduces the excitatory response to 5-HT. H-9 Dihydrochloride also has a direct effect on pharyngeal activity. H-9 Dihydrochloride inhibits signal-transduction and cell growth in EGF (epidermal growth factor)-dependent epithelial cell lines.
    H-9 Dihydrochloride
  • HY-124821
    VA012
    		Modulator 99.34%
    VA012 (compound 11) is a positive allosteric modulator (PAM) of the serotonin 5-HT2C receptor. VA012 reduces food intake and body weight gain without causing CNS-related malaise during subchronic administration. VA012 can be utilized in obesity research.
    VA012
  • HY-121208
    Ketanserinol
    		Antagonist 98.05%
    Ketanserinol (R 46742) is a metabolite of Ketanserin (HY-10562). Ketanserinol is a competitive antagonist of the effects of 5-HT (HY-B1473A) in both arteries. The KB values are 6.5 for large coronary arteries and 6.4 for pulmonary arteries.
    Ketanserinol
  • HY-W050162
    (E)-3,4,5-Trimethoxycinnamic acid
    		Inhibitor 99.95%
    (E)-3,4,5-Trimethoxycinnamic acid (TMCA) is a cinnamic acid substituted by multi-methoxy groups. (E)-3,4,5-Trimethoxycinnamic acid is an orally active and potent GABAA/BZ receptor agonist. (E)-3,4,5-Trimethoxycinnamic exhibits favourable binding affinity to 5-HT2C and 5-HT1A receptor, with IC50 values of 2.5 and 7.6 μM, respectively. (E)-3,4,5-Trimethoxycinnamic acid shows anticonvulsant and sedative activity. (E)-3,4,5-Trimethoxycinnamic acid can be used for the research of insomnia, headache and epilepsy.
    (E)-3,4,5-Trimethoxycinnamic acid
  • HY-103415
    Nemonapride
    		Agonist 99.90%
    Nemonapride is a highly potent dopamine D2 receptor antagonist with a Ki of 0.06 nM. Nemonapride also activates 5-HT1A receptor with an IC50 of 34 nM. Nemonapride is an antipsychotic that readily passes through the blood brain barrier and exhibits potent neuroleptic effects in animals.
    Nemonapride
  • HY-121793
    Roemerine
    		99.61%
    Roemerine is an alkaloid that has been identified from the leaves of Fibraurea recisa Pierre. Roemerine exhibits antibacterial, anticancer, and antidepressant activities, can reverse the multidrug resistance phenotype in cultured cells, and exerts antibacterial effects by regulating the cAMP signaling pathway. Additionally, Roemerine influences neuronal activity by increasing BDNF protein expression and modulating the serotonergic and glutamatergic systems. Roemerine holds promise for research in the fields of cancer, infections, and neurological diseases.
    Roemerine
  • HY-12959A
    Repinotan hydrochloride
    		Agonist
    Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects.
    Repinotan hydrochloride
  • HY-125641
    AL-34662
    		Agonist 99.19%
    AL-34662 is a selective 5-HT2A receptoragonist (IC50: 0.77 nM and 1.5 nM for rat and human 5-HT2 receptor). AL-34662 is also a weak α-1D adrenergic agonist activity (EC50:0.4 μM). AL-34662 is an ocular hypotensive agent.
    AL-34662
  • HY-14147
    Renzapride
    		Agonist 98.36%
    Renzapride (BRL 24924), a substituted benzamide, is a full 5-HT4 receptor agonist with a Ki value of 115 nM. Renzapride (BRL 24924) is also a 5HT2b and 5HT3 receptor antagonist. Renzapride could be used for constipation predominant irritable bowel syndrome (C-IBS) study.
    Renzapride
  • HY-110023
    Zimelidine dihydrochloride
    		Inhibitor 98.27%
    Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin 5-HT uptake and SERT. Zimelidine dihydrochloride is an antidepressant.
    Zimelidine dihydrochloride
  • HY-14958A
    Pardoprunox hydrochloride
    		Agonist 99.46%
    Pardoprunox (SLV-308) hydrochloride is a partial dopamine D2 and D3 receptor partial agonist and a serotonin 5-HT1A receptor agonist, with pEC50s of 8, 9.2, and 6.3, respectively.
    Pardoprunox hydrochloride
  • HY-B0002S
    Ondansetron-d3 hydrochloride
    		Antagonist 98.78%
    Ondansetron-d3 (hydrochloride) is the deuterium labeled Ondansetron hydrochloride. Ondansetron hydrochloride (GR 38032 hydrochloride) is a serotonin 5-HT3 receptor antagonist used mainly as anantiemetic (to treat nausea and vomiting), often following chemotherapy[1][2].
    Ondansetron-d<sub>3</sub> hydrochloride
  • HY-100649
    Hydroxy ziprasidone
    		Antagonist 99.53%
    Hydroxy ziprasidone is an impurity of Ziprasidone. Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist.
    Hydroxy ziprasidone
  • HY-B0031S
    Quetiapine-d4 fumarate
    		Agonist ≥98.0%
    Quetiapine-d4 (fumarate) is the deuterium labeled Quetiapine fumarate. Quetiapine fumarate is a 5-HT receptors agonist and a dopamine receptor antagonist. Antidepressant and anxiolytic effects[1].
    Quetiapine-d<sub>4</sub> fumarate
  • HY-110033
    Ecopipam hydrobromide
    		Antagonist ≥99.0%
    Ecopipam (SCH 39166) hydrobromide is a potent, selective and orally active antagonist of dopamine D1/D5 receptor, with Kis of 1.2 nM and 2.0 nM, respectively. Ecopipam hydrobromide shows more than 40-flod selectivity over D2, D4, 5-HT, and α2a receptor (Ki=0.98, 5.52, 0.08, and 0.73 μM, respectively). Ecopipam hydrobromide can be used for the research of schizophrenia and obesity.
    Ecopipam hydrobromide
  • HY-14543S
    Sertindole-d4
    		Antagonist 98.64%
    Sertindole-d4 is the deuterium labeled Sertindole. Sertindole, a neuroleptic, is one of the newer antipsychotic medications available[1][2].
    Sertindole-d<sub>4</sub>
  • HY-101924
    AVN-492
    		Antagonist 99.30%
    AVN-492 is a very specific and highly-selective antagonist with picomolar affinity to 5-HT6R (Ki=91 pM).
    AVN-492
  • HY-116565
    Usmarapride
    		Modulator ≥98.0%
    Usmarapride (SUVN-D4010) is a potent, selective, orally active and brain penetrant 5-HT4 receptor partial agonist (EC50=44 nM). Usmarapride (SUVN-D4010) can be used for the research of cognitive deficits associated with Alzheimer's disease.
    Usmarapride
  • HY-17382B
    Metoclopramide hydrochloride
    		Antagonist 99.96%
    Metoclopramide hydrochloride is a potent and orally active antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide hydrochloride can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.
    Metoclopramide hydrochloride
  • HY-B0189B
    Mosapride citrate dihydrate
    		Agonist
    Mosapride (TAK-370) citrate dehydrate is a gastroprokinetic agent with 5-hydroxytryptamine4 receptor agonist activity and has been widely used in the research of a variety of gastrointestinal disorders. Mosapride citrate dihydrate potently inhibits Kv4.3 in a concentration-dependent manner with IC50 values of 15.2 μM. Mosapride citrate dihydrateselectively stimulates upper GI motility in vivo.
    Mosapride citrate dihydrate
Cat. No. Product Name / Synonyms Application Reactivity