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

5-HT Receptor

Serotonin Receptor; 5-hydroxytryptamine Receptor

5-HT Receptor

Related Products

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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-101365A
    RS-102221 hydrochloride
    		Antagonist 99.33%
    RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats.
    RS-102221 hydrochloride
  • HY-123205
    Oxatomide
    		Inhibitor 99.56%
    Oxatomide is a potent and orally active dual H1-histamine receptor and P2X7 receptor antagonist with antihistamine and anti-allergic activity. Oxatomide almost completely blocks the ATP-induced current in human P2X7 receptors (IC50 of 0.95 μM). Oxatomide inhibits ATP-induced Ca2+ influx with an IC50 value of 0.43 μM and also inhibits serotonin.
    Oxatomide
  • HY-100820
    Sarizotan
    		Agonist 98.74%
    Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.
    Sarizotan
  • 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-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-103151
    CP94253 hydrochloride
    		Agonist 98.84%
    CP94253 hydrochloride is a potent and selective agonist of 5-HT1B receptor (Ki= 2 nM in a radioligand binding assay).Ki values for 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors are 89, 49, 860, and 1600 nM respectively. CP94253 hydrochloride is centrally active upon systemic administration in vivo.
    CP94253 hydrochloride
  • HY-103142
    AS19
    		Agonist 99.85%
    AS19 is a potent, selective 5-HT7 receptor agonist with an IC50 value of 0.83 nM and a Ki of 0.6 nM. AS19 is selective for 5-HT7 over 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A receptors (Kis = 89.7 nM, 490 nM, 6.6 nM and 98.5 nM, respectively). AS19 enhances memory consolidation and reverses Scopolamine- or Dizocilpine-induced amnesia.
    AS19
  • HY-90003A
    Tianeptine sodium salt
    		Agonist 99.90%
    Tianeptine sodium salt is a selective facilitator of 5-HT uptake. Tianeptine sodium salt has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine sodium salt has antidepressant, anxiolytic, analgesic and neuroprotective activities.
    Tianeptine sodium salt
  • 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-13788
    LY 344864
    		Agonist 98.93%
    LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. LY 344864 is a full agonist producing an effect similar in magnitude to serotonin itself. LY 344864 can cross the blood brain barrier to some extent.
    LY 344864
  • 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-32329
    Setiptiline
    		Modulator 98.03%
    Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
    Setiptiline
  • 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-14537
    Latrepirdine dihydrochloride
    		Antagonist 99.65%
    Latrepirdine dihydrochloride is a neuroactive compound with antagonist activity at histaminergic, α-adrenergic, and serotonergic receptors. Latrepirdine stimulates amyloid precursor protein (APP) catabolism and amyloid-β (Aβ) secretion.
    Latrepirdine dihydrochloride
  • 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-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-19889
    JNJ-18038683
    		Antagonist 99.76%
    JNJ-18038683 is a 5-Hydroxytryptamine Type 7 (5-HT7) receptor antagonist, with pKis of 8.19, 8.20 for rat and human 5-HT7 in HEK293 cells, respectively.
    JNJ-18038683
  • 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-B0500
    Alverine citrate
    		Antagonist 99.71%
    Alverine citrate is a 5-HT1A receptor antagonist, with an IC50 of 101 nM.
    Alverine citrate
  • HY-B1165
    Cyproheptadine hydrochloride sesquihydrate
    		Antagonist 99.82%
    Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
    Cyproheptadine hydrochloride sesquihydrate
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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