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-B1115A
    Buspirone
    		Agonist 99.86%
    Buspirone is an orally active 5-HT1A receptor agonist, and a dopamine D2 autoreceptorsant antagonist. Buspirone is an anxiolytic agent, and can be used for the generalized anxiety disorder research.
    Buspirone
  • HY-10564
    Sarpogrelate hydrochloride
    		Antagonist 99.09%
    Sarpogrelate hydrochloride (MCI-9042) is a selective 5-HT2R antagonist, with pKis of 8.52, 6.57, and 7.43 for 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. Sarpogrelate hydrochloride displays selectivity over 5-HT1, 5-HT3, 5-HT4, α1-, α2- and β-adrenoreceptor, histamine H1, H2 and muscarinic M3 receptors. Sarpogrelate hydrochloride can be used for the research of vascular disease associated with thrombosis.
    Sarpogrelate hydrochloride
  • HY-W019599
    4-Chloro-L-phenylalanine
    		Inhibitor ≥98.0%
    4-Chloro-L-phenylalanine (L-PCPA) is a 5-HT biosynthesis inhibitor. 4-Chloro-L-phenylalanine is also a nonspecific antagonist of both isoforms of tryptophan hydroxylase (TPH1 and TPH2).
    4-Chloro-L-phenylalanine
  • HY-103156
    NAS-181 dimesylate
    		Antagonist 98.44%
    NAS181 is a potent and selective antagonist of rat 5-HT1B receptor, with a Ki of 47 nM. NAS181 shows 13-fold selectivity for r5-HT1B over bovine 5-HT1B receptor (Ki=630 nM). NAS181 increases the 5-HT turnover and the synaptic concentration of 5-HT by inhibiting terminal r5-HT1B autoreceptors.
    NAS-181 dimesylate
  • HY-32329A
    Setiptiline maleate
    		Antagonist 99.94%
    Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate 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 maleate
  • 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-N0740
    Jatrorrhizine chloride
    		Inhibitor 99.88%
    Jatrorrhizine chloride is an alkaloid isolated from?Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine chloride is a potent and orally active inhibitor of?AChE?(IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine chloride reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.
    Jatrorrhizine chloride
  • HY-A0010
    Eletriptan hydrobromide
    		Agonist 99.81%
    Eletriptan hydrobromide (Eletriptan HBr) is a 5-HT1B and 5-HT1D receptor agonist with antimigraine activity, with Ki of 0.92 nM and 3.14 nM, respectively.
    Eletriptan hydrobromide
  • HY-B0071
    Granisetron
    		Antagonist 99.95%
    Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
    Granisetron
  • HY-B1622
    Cyproheptadine
    		Antagonist 99.86%
    Cyproheptadine is a potent and orally active 5-HT2A receptor antagonist, with antidepressant and antiserotonergic effects. Cyproheptadine has antiplatelet and thromboprotective activities. Cyproheptadine can be used for the research of thromboembolic disorders.
    Cyproheptadine
  • HY-17382
    Metoclopramide
    		Antagonist 99.94%
    Metoclopramide is a potent antagonist of 5-HT3 and dopamine D2 receptor, with IC50s of 308 nM and 483 nM, respectively. Metoclopramide can be used for the research of nausea and vomiting, gastro-oesophageal reflux, and gastroparesis.
    Metoclopramide
  • HY-109157
    Ralmitaront
    		Agonist 99.92%
    Ralmitaront (RO6889450) is an orally active agonist of trace amine-associated receptor 1 (TAAR1) with a EC50 value of 110.4 nM. Ralmitaront has antipsychotic, cognitively improvement, and antidepressant activity in rodents. Ralmitaront can be used as a neurosuppressant in the study of neuro-related diseases, such as schizophrenia (SCZ), schizoaffective disorder.
    Ralmitaront
  • HY-B0478A
    Trazodone
    		Antagonist 99.84%
    Trazodone (AF-1161 free base) is a serotonin receptor antagonist and reuptake inhibitor. Trazodone can be used for the research of major depressive disorder. Trazodone also has potential for sleep disorder research.
    Trazodone
  • HY-10847B
    SB-277011 hydrochloride
    		Antagonist 98.54%
    SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate?dopamine D3?receptor (D3R)?antagonist with Ki values of 10.7?nM and?11.2 nM?at?rodent and human?D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with?pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
    SB-277011 hydrochloride
  • HY-B0071A
    Granisetron Hydrochloride
    		Antagonist 99.87%
    Granisetron (Hydrochloride) (BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
    Granisetron Hydrochloride
  • HY-19358
    2-Methyl-5-HT
    		Agonist 98.73%
    2-Methyl-5-HT (2-Methyl-5-hydroxytryptamine) is a potent and selective 5-HT3 receptor agonist. 2-Methyl-5-HT is shown to display anti-depressive-like effects.
    2-Methyl-5-HT
  • HY-W011235
    Norfluoxetine hydrochloride
    		Inhibitor 99.58%
    Norfluoxetine hydrochloride is an active N-demethylated metabolite of Fluoxetine. Fluoxetine is a selective serotonin (5-HT) reuptake inhibitor that is metabolized to Norfluoxetine hydrochloride by cytochrome P450 (CYP) 2D6, CYP2C19, and CYP3A4. Norfluoxetine hydrochloride inhibits 5-HT uptake and inhibits CaV3.3 T current (IC50 = 5 μM). Norfluoxetine hydrochloride has anticonvulsant activity.
    Norfluoxetine hydrochloride
  • HY-19733
    Lumateperone tosylate
    		Antagonist 99.53%
    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
  • 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 (SB 207266) is a 5-HT4 selective inhibitor of the serotonin receptor.
    Piboserod
Cat. No. Product Name / Synonyms Application Reactivity
5-HT Receptor Isoform Comparison

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