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-19863
    F-15599
    		Agonist 99.82%
    F-15599 is a highly selective G-protein biased 5-HT1A receptor agonist, with Ki of 3.4 nM.
    F-15599
  • HY-W028142
    Quipazine
    		Agonist
    Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research.
    Quipazine
  • HY-111385
    UNC9994 hydrochloride
    		Modulator 98.83%
    UNC9994 hydrochloride is a functionally selective, β-arrestin–biased dopamine D2 receptor (D2R) agonist that selectively activates β-arrestin recruitment and signaling. UNC9994 hydrochloride shows a binding affinity with a Ki of 79 nM for D2R. UNC9994 hydrochloride is also an antagonist of Gi-regulated cAMP production and partial agonist for D2R/β-arrestin-2 interactions. UNC9994 hydrochloride shows antipsychotic-like activity.
    UNC9994 hydrochloride
  • HY-10121
    Asenapine
    		Antagonist 99.62%
    Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4) and histamine receptors (pKi: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.
    Asenapine
  • HY-15574
    Piboserod
    		Antagonist 99.09%
    Piboserod is an orally available selective antagonist of the 5-HT4 receptor, with a Ki value of approximately 0.1 nM for human 5-HT4 receptors. Piboserod can competitively bind to the 5-HT4 receptor and block the activation of the 5-HT4 receptor. Piboserod can inhibit the enhancing effect of 5-HT on the nerve-mediated contraction response of the human bladder detrusor muscle. Piboserod is mainly used in the research of urinary system diseases (such as overactive bladder) and cardiovascular diseases (such as chronic heart failure).
    Piboserod
  • HY-B1059
    Levosulpiride
    		Antagonist 99.88%
    Levosulpiride (RV-12309) is the (S)-enantiomer of sulpiride, which is a D2 receptor a antagonist, an atypical antipsychotic agent of the benzamide class.
    Levosulpiride
  • HY-103137
    Zacopride hydrochloride
    		99.69%
    Zacopride hydrochloride is an orally active 5-HT3 receptor (Ki of 0.38 nM) antagonist and 5-HT4 receptor (Ki of 373 nM) agonist. Zacopride hydrochloride exhibits multiple activities, such as regulating gastrointestinal motility, affecting cardiac function, and exerting anxiolytic and antiemetic effects. Zacopride hydrochloride is currently mainly used in the research of gastrointestinal diseases, cardiovascular diseases, and psychiatric diseases such as anxiety.
    Zacopride hydrochloride
  • HY-30152
    Xanthotoxol
    		Antagonist 99.75%
    Xanthotoxol (8-Hydroxypsoralen) It is a kind of fragrant bean substance, and it is a CYP450 inhibitor. Xanthotoxol has anti-inflammatory, anti-inflammatory, and 5-HT antagonistic and protective effects. Xanthotoxol inhibited CYP3A4 sum CYP1A2 IC50s separation 7.43 μM sum 27.82 μM. Xanthotoxol can pass through MAPK and NF-κB, inhibiting inflammation.
    Xanthotoxol
  • HY-A0019A
    Paliperidone palmitate
    		Antagonist 98.41%
    Paliperidone palmitate is an orally effective competitive antagonist of dopamine D2 receptors and 5-hydroxytryptamine 2A (5-HT2A) receptors that can cross the blood-brain barrier. Paliperidone palmitate competitively inhibits the effects of dopamine and 5-hydroxytryptamine by binding to dopamine D2 receptors and 5-HT2A receptors, regulating the balance of the neurotransmitter system and thus exerting antipsychotic activity. Paliperidone palmitate is mainly used in the research field of schizophrenia.
    Paliperidone palmitate
  • HY-118010A
    (+)-Norfenfluramine hydrochloride
    		Agonist 99.77%
    (+)-Norfenfluramine hydrochloride, a major hepatic metabolite of (+)-fenfluramine, is a selective 5-HT2B receptor agonist (Ki: 11.2 nM). (+)-Norfenfluramine hydrochloride potently stimulates the hydrolysis of inositol phosphates and increases intracellular Ca2+. (+)-Norfenfluramine hydrochloride can be used for the research of primary pulmonary hypertension and valvular heart disease.
    (+)-Norfenfluramine hydrochloride
  • HY-17410
    Iloperidone
    		Antagonist 99.97%
    Iloperidone (HP 873) is a D2/5-HT2 receptor antagonist. Iloperidone is an atypical antipsychotic for the schizophrenia symptoms.
    Iloperidone
  • HY-13221
    BRL 54443
    		Agonist 98.97%
    BRL 54443 is a potent 5-HT1E/1F receptor agonist (Ki values are 1.1 nM and 0.7 nM respectively); displays > 30-fold selectivity over other 5-HT and dopamine receptors.
    BRL 54443
  • HY-B0031
    Quetiapine hemifumarate
    		Agonist 99.94%
    Quetiapine hemifumarate is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine hemifumarate is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine hemifumarate has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.25, 5.74, 7.54, 5.55. Antidepressant and anxiolytic effects.
    Quetiapine hemifumarate
  • HY-B0020
    Tropisetron Hydrochloride
    		Antagonist 99.97%
    Tropisetron Hydrochloride (SDZ-ICS-930) is an effective neuroprotective agent that acts as a 5-HT3 receptor antagonist, a calmodulin inhibitor, and an α7-nAChRreceptor agonist, with an IC50 of 70.1 nM for the 5-HT3 receptor. Tropisetron Hydrochloride has anti-inflammatory properties and immune-regulating functions, effectively alleviating symptoms associated with chemotherapy and post-surgery. Tropisetron Hydrochloride reduces Ab (HY-P4867)-induced hippocampal neuroinflammation.
    Tropisetron Hydrochloride
  • HY-U00443
    SB 258719
    		Antagonist 99.04%
    SB 258719 is a selective 5-HT7 receptor antagonist with high affinity (pKi=7.5) for the receptor. SB 258719 can be used for the research of cancer and neurological disease.
    SB 258719
  • HY-W015169
    5-Methoxytryptamine
    		Agonist 99.91%
    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
  • HY-101331
    Phenylbiguanide
    		Agonist ≥98.0%
    Phenylbiguanide is a 5-HT3 receptor selective agonist with an EC50 of 3.0±0.1 μM.
    Phenylbiguanide
  • HY-B0595
    Ramosetron Hydrochloride
    		Antagonist 99.96%
    Ramosetron (YM060 free base) Hydrochloride is an orally active 5-HT3 antagonist that improves dysphoria, interference with activity and food avoidance. Ramosetron Hydrochloride is promising for research of irritable bowel syndrome with diarrhea.
    Ramosetron Hydrochloride
  • HY-101341
    RS 67333 hydrochloride
    		Agonist 99.73%
    RS 67333 hydrochloride is a potent and selective 5-HT4 receptor (5-HT4R) partial agonist with a pKi of 8.7 in guinea-pig striatum. RS 67333 hydrochloride exhibits lower affinities at several other receptors including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2 and muscarinic M1-M3 receptors. RS 67333 hydrochloride has neuroprotective effects, and can be used for Alzheimer's disease research.
    RS 67333 hydrochloride
  • HY-103101
    LP44 hydrochloride
    		Agonist 98.06%
    LP44 (hydrochloride) is a selective 5-HT7 agonist with Ki of 0.22 nM. LP44 (hydrochloride) induces hypothermic effect in a dose-dependent manner by intracerebroventricular injection. LP44 (hydrochloride) not causes considerable hypothermic response by intraperitoneal administration.
    LP44 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity