5-HT Receptor
Serotonin Receptor; 5-hydroxytryptamine Receptor
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
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5-HT Receptor
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5-HT1 Receptor
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5-HT2 Receptor
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5-HT3 Receptor
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5-HT4 Receptor
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5-HT5 Receptor
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5-HT6 Receptor
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5-HT7 Receptor
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All Product Categories
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5-HT Receptor Inhibitors
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5-HT Receptor Agonists
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5-HT Receptor Antagonists
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5-HT Receptor Activators
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5-HT Receptor Modulators
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5-HT Receptor Inducers
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5-HT Receptor Controls
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5-HT Receptor Ligands
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5-HT Receptor Related Products (1729)
Related Products (1729)
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Antibodies (1)
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Related Compound Screening Libraries (1)
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5-HT Receptor Isoform Comparison
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Gamma-Mangostin
0 ImagesSynonyms: γ-MangostinGamma-Mangostin is a novel competitive 5-hydroxytryptamine 2A (5-HT2A) receptor antagonist and potent epoxidase 2 (COX-2) inhibitor, as well as a transthyroxin protein (TTR) profibrosis inhibitor. Gamma-Mangostin binds to the thyroxine (T4)-binding sites and stabilized the TTR tetramer. Gamma-Mangostin inhibits [3H] spiperone binding to cultured rat aortic myocytes (IC50=3.5 nM) and reduces The perfusion pressure response of rat coronary artery to 5-HT2A (IC50=0.32 μM). Gamma-Mangostin has anti-inflammatory, antibacterial, antioxidant and anticancer activities, and can be used in the study of metabolic disorders such as diabetes.
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Bretisilocin
0 ImagesSynonyms: GM-2505Bretisilocin (GM-2505) is the agonist for 5-HT2A receptor and a serotonin releaser. Bretisilocin exhibits antidepressant activity and can be used in the study of depression.
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Ondansetron hydrochloride dihydrate
0 ImagesSynonyms: GR 38032 hydrochloride dihydrate; SN 307 hydrochloride dihydrateOndansetron (GR 38032; SN 307) hydrochloride dehydrate is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride dehydrate exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride dehydrate can inhibit nausea and vomiting induced by chemotherapy and radiotherapy.
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EEDQ
0 ImagesSynonyms: EEDQEEDQ is a carboxylate activator and irreversible antagonist of 5HT2c receptors. EEDQ reduces [3H]β-CIT binding to the dopamine transporter (DAT) in rat caudate-putamen (CPu) homogenates (IC50 = 78.3 μM). EEDQ inhibits contralateral rotation behavior.
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8-OH-DPAT hydrobromide
0 ImagesSynonyms: 8-Hydroxy-DPAT hydrobromide8-OH-DPAT (8-Hydroxy-DPAT) hydrobromide is a potent, brain-penetrant and selective 5-HT1A agonist with a pIC50 of 8.19. 8-OH-DPAT hydrobromide has selectivity of almost 1000 fold for a subtype of the 5-HT1 binding site.
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Asenapine maleate
0 ImagesSynonyms: Org 5222 maleateAsenapine (Org 5222) maleate, a brain-penetrant 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 maleate can be used in the research of schizophrenia and bipolar disorder.
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Tegaserod
0 ImagesTegaserod is an orally active serotonin receptor 4 (HTR4; 5-HT4R) agonist and a 5-HT2B receptor antagonist. Tegaserod has pKis of 7.5, 8.4 and 7.0 for human recombinant 5-HT2A, 5-HT2B and 5-HT2C receptors, respectively. Tegaserod causes tumor cell apoptosis, blunts PI3K/Akt/mTOR signaling and decreases S6 phosphorylation. Tegaserod has anti-tumor activity and has the potential for irritable bowel syndrome (IBS) research.
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Gepirone
0 ImagesGepirone is a selective and affinitive 5-HT1A agonist. Gepirone binds selectively to 5-HT1A receptor binding site. Gepirone acts as an antidepressant agent can be used for anxiety and major depressive disorder research.
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Loxapine succinate
0 ImagesLoxapine succinate is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent. Loxapine can also suppresses bacterial efflux pump activity and inhibit intracellular multiple-antibiotic-resistant Salmonella enterica serovar Typhimurium in macrophages.
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Blonanserin
0 ImagesSynonyms: AD-5423Blonanserin (AD-5423) is a potent and orally active 5-HT2A (Ki=0.812 nM) and dopamine D2 receptor (Ki =0.142 nM) antagonist. Blonanserin is usually acts as an atypical antipsychotic agent and can be used for the research of extrapyramidal symptoms, excessive sedation, or hypotension.
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SB-699551
0 ImagesSB-699551 is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 can be used for the research of anxiety, breast cancer, and Alzheimer's disease.
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SB-224289 hydrochloride
0 ImagesSynonyms: SB-224289ASB-224289 hydrochloride is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
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Metergoline
0 ImagesMetergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na+ channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation.
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Levomepromazine
0 ImagesLevomepromazine (Methotrimeprazine) is an orally active antipsychotic compound and Ca2+ release inducer. Levomepromazine inhibits SERCA pump and induces an increase in cytoplasmic Ca2+ levels. Levomepromazine has antagonistic effects on a variety of neurotransmitter receptors, including dopamine, cholinergic, serotonin, and histamine receptors. Levomepromazine can induce adaptive ER stress and autophagy. In addition, Levomepromazine has antiviral, anti-inflammatory, neuroprotective and analgesic, sedative and anti-injurious activities. Levomepromazine can be used in the study psychiatric disorders and relieving nausea and vomiting.
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Granisetron
0 ImagesSynonyms: BRL 43694Granisetron (BRL 43694) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
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Ketanserin tartrate
0 ImagesSynonyms: R41468 tartrateKetanserin (R41468) tartrate is a selective 5-HT2 receptor antagonist. Ketanserin tartrate also blocks hERG current (IhERG) in a concentration-dependent manner (IC50=0.11 μM).
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Ecopipam hydrochloride
0 ImagesSynonyms: SCH 39166 hydrochlorideEcopipam (SCH 39166) hydrochloride 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 hydrochloride 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 hydrochloride can be used for the research of schizophrenia and obesity.
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2-Methyl-5-HT
0 ImagesSynonyms: 2-Methyl-5-hydroxytryptamine; 2-Methylserotonin; 2-Me-5-HT2-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.
