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.

5-HT Receptor Isoform Specific Products:

5-HT Receptor Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-109067A
    Opiranserin hydrochloride
    		Antagonist 99.62%
    Opiranserin (VVZ-149) hydrochloride, a non-opioid and non-NSAID analgesic candidate, is a dual antagonist of glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), with IC50s of 0.86 and 1.3 μM, respectively. Opiranserin hydrochloride shows antagonistic activity on rP2X3 (IC50=0.87 μM). Opiranserin hydrochloride is development as an injectable agent for the treatment of postoperative pain.
    Opiranserin hydrochloride
  • HY-A0095
    Flibanserin
    		Modulator 99.43%
    Flibanserin (BIMT-17; BIMT-17BS) is an orally active serotonin 5-HT1A receptor agonist and 5-HT2A receptor antagonist with Ki values of 1 nM and 49 nM, respectively. Flibanserin binds to dopamine D4 receptors with an Ki value of 4-24 nM. Flibanserin shows anti-depression and anti-anxiety effect, can be used to hypoactive sexual desire disorder (HSDD) research-.
    Flibanserin
  • HY-103102
    TCB2
    		Agonist 99.21%
    TCB2 is an agonist of serotonin 5-HT2A receptor.
    TCB2
  • 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-B0750
    Dolasetron
    		Antagonist ≥98.0%
    Dolasetron(MDL-73147) is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy.
    Dolasetron
  • HY-17637
    Lumateperone
    		99.83%
    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
  • HY-B0072
    Tropisetron
    		Antagonist 99.93%
    Tropisetron is an orally active 5-HT3R antagonist (Ki = 5.3 nM) as well as being a potent and selective α7 nicotinic partial agonist (EC50 = 1.3 μM). Tropisetron prevents phosphorylation and activation of the p38 MAPK. Tropisetron inhibits both IL-2 gene transcription and IL-2 synthesis in stimulated T cells. Tropisetron inhibits the binding to DNA and the transcriptional activity of NFAT and AP-1. Tropisetron is anti-inflammatory and antiemetic. Tropisetron has antitumor and neuroprotective effects. Tropisetron can be studied in research for diseases including hemorrhagic cystitis, chronic joint inflammation, lung cancer and chronic cerebral hypoperfusion.
    Tropisetron
  • HY-B0031
    Quetiapine hemifumarate
    		Agonist 99.96%
    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-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-100938
    m-CPBG hydrochloride
    		Agonist 99.78%
    m-CPBG (1-(3-Chlorophenyl)biguanide) hydrochloride is a selective 5-HT3 agonist. m-CPBG hydrochloride can be used for the research of neurological disease.
    m-CPBG hydrochloride
  • HY-13527
    LY310762
    		Antagonist 98.68%
    LY310762 is a selective 5-HT1D receptor antagonist (Ki=249 nM) with a weak affinity for 5-HT1B receptor. LY310762 effectively abolishes the renal vasodilatory effects of 5-HTSumatriptan (HY-B0121B)-induced decrease in excitatory postsynaptic potential (EPSC) amplitude.
    LY310762
  • HY-100554
    BMY 7378
    		Agonist 99.92%
    BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist.
    BMY 7378
  • 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 99.46%
    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-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-123205
    Oxatomide
    		Inhibitor 98.11%
    Oxatomide (KW-4354) is an orally active dual antagonist of the H1-histamine receptor and the P2X7 receptor, as well as an inhibitor of serotonin. Oxatomide possesses antihistaminic, antiallergic and anti-inflammatory activities. Oxatomide can be used in the research of allergic diseases.
    Oxatomide
  • HY-17407
    Ziprasidone hydrochloride monohydrate
    		Antagonist 98.11%
    Ziprasidone (CP-88059) hydrochloride monohydrate is an orally active combined 5-HT and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM).
    Ziprasidone hydrochloride monohydrate
  • HY-19733
    Lumateperone tosylate
    		Antagonist 99.78%
    Lumateperone (ITI-007) tosylate is a 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 tosylate has anticancer activity and can also be used in studies of psychiatric disorders such as schizophrenia.
    Lumateperone tosylate
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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