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
(35)
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5-HT4 Receptor
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5-HT5 Receptor
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5-HT6 Receptor
(86)
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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 (1773)
Related Products (1773)
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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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Asenapine-13C,d3
0 ImagesCat. No.: HY-10121S2CAS No.: 2747915-30-4Synonyms: Org 5222-13C,d3Asenapine-13C,d3 is 13C and deuterated labeled Asenapine (HY-10121). 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.
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MT-1207 free base
0 ImagesCat. No.: HY-187975CAS No.: 917613-59-3MT-1207 free base is an orally active, selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 has IC50 values of <0.1 nM, 0.15 nM, 1.40 nM, and 0.27 nM for α1A, α1B, α1D, and 5-HT2A, respectively. MT-1207 free base induces vasodilation, improves baroreflex sensitivity, and reduces heart rate in isolated hearts. MT-1207 free base lowers blood pressure, protects the heart, brain, and kidneys, improves cognition, delays stroke, reduces mortality, and lowers uric acid without impairing renal function in SHR/2K1C/2K2C models. MT-1207 free base exhibits high plasma protein binding, resistance to plasma esterases, and NADPH-dependent hepatic metabolism. MT-1207 free base can be used for research related to hypertension.
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AS2030680
0 ImagesCat. No.: HY-182695CAS No.: 2170562-35-1AS2030680 is a blood-brain barrier-permeable, orally active 5-HT5A receptor antagonist. AS2030680 regulates 5-HT5A-related downstream signaling pathways, reduces the frequency of tumorsphere-initiating cells in breast cancer cells, and exerts procognitive activity in animal models. AS2030680 can be used to study cognitive impairments associated with dementia and schizophrenia, as well as breast cancer.
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LY-426965 hydrochloride
0 ImagesCat. No.: HY-117799ACAS No.: 326821-27-6LY-426965 hydrochloride is a potent arylpiperazine compound known for its role as a full antagonist of the serotonin 1A receptor, lacking partial agonist activity. It is identified as a selective 5-HT1A antagonist, showing promise in preclinical studies for treating conditions associated with serotonin dysregulation, such as smoking cessation and depression-related disorders.
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SUVN-507
0 ImagesCat. No.: HY-18276CAS No.: 959395-84-7SUVN-507 is a 5-HT6 receptor antagonist. SUVN-507 can reverse cognitive impairments and enhance excitatory neural transmission while weakening inhibitory neural transmission. SUVN-507 can be used for the research of neurological disease, such as Alzheimer's disease.
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PRX-08066 maleate
0 ImagesCat. No.: HY-15472ACAS No.: 866206-55-5PRX-08066 maleate is a selective and orally active 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist with a Ki of 3.4 nM. PRX-08066 maleate inhibits the MAPK pathway, 5-HT release and fibrotic factor (TGFβ1, CTGF and FGF2) expression. PRX-08066 maleate inhibits the proliferation of KRJ-I cells and induces apoptosis (caspase-3 activation). PRX-08066 maleate inhibits pulmonary vascular remodeling. PRX-08066 maleate can be used of pulmonary Arterial Hypertension (PAH) and neuroendocrine tumor (NET).
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Methiothepin
0 ImagesCat. No.: HY-111491CAS No.: 20229-30-5Synonyms: Metitepine; Ro 8-6837Methiothepin (Metitepine; Ro 8-6837) is a potent and non-selective 5-HT2 receptor antagonist, with pKds of 7.10 (5-HT1A), 7.28 (5HT1B), 7.56 (5HT1C), 6.99 (5HT1D), 7.0 (5-HT5A), 7.8 (5-HT5B), 8.74 (5-HT6), and 8.99 (5-HT7), and pKis of 8.50 (5HT2A), 8.68 (5HT2B), and 8.35 (5HT2C).
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SB-224289
0 ImagesCat. No.: HY-101105CAS No.: 180083-23-2SB-224289 is a selective 5-HT1B receptor antagonist, with anxiolytic effect.
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AVN-322 free base
0 ImagesCat. No.: HY-107125ACAS No.: 1194574-33-8AVN-322 free base is an orally active, highly selective 5-HT6Rantagonist for central nervous system disease research.
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GSK215083
0 ImagesCat. No.: HY-118836CAS No.: 607742-80-3GSK215083 is a high affinity 5-HT6 receptor antagonist. GSK215083 can serves as a promising 5-HT6 radioligand candidate by radiolabeled with (11)C via methylation.
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Hordenine-d6 hydrochloride
0 ImagesCat. No.: HY-N0113BSSynonyms: Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochlorideHordenine-d6 hydrochloride (Ordenina-d6 hydrochloride; Peyocactine-d6 hydrochloride) is the deuterated-labeled Hordenine hydrochloride (HY-N0113B). Hordenine hydrochloride (Ordenina hydrochloride; Peyocactine hydrochloride) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine hydrochloride inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine hydrochloride inhibits melanin synthesis in melanocytes and reconstructed epidermis. Hordenine hydrochloride activates the Wnt/β-catenin signaling pathway. Hordenine hydrochloride activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine hydrochloride inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine hydrochloride limits alcohol intake, reduces relapse drinking behavior. Hordenine hydrochloride can be used for research on mastitis, skin pigmentation, acute lung injury, foodborne diseases, hair loss, Parkinson's disease, bacterial infections, and alcohol use disorder.
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KB R6933
0 ImagesCat. No.: HY-105449ACAS No.: 148565-09-7Synonyms: KB 6806 maleate
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Wf-516 hydrochloride
0 ImagesCat. No.: HY-19417CAS No.: 310392-93-9Wf-516 hydrochloride is an inhibitor of 5-HT reuptake, and an antagonist of 5-HT1A and 5-HT2A receptors, with Ki of 5 nM and 40 nM for 5-HT1A receptor and 5-HT2A receptor in humans, respectively.Wf-516 hydrochloride has potent antidepressant activity.
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5-HT2A antagonist 3
0 ImagesCat. No.: HY-171235CAS No.: 1134815-69-25-HT2A antagonist 3 (Formula (III)) is a 5-HT2A receptor antagonist and inverse agonist with a pIC50 of 8.7 and a pKi of 9. 5-HT2A antagonist 3 can be utilized in neurological reesearch.
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Pruvanserin hydrochloride
0 ImagesCat. No.: HY-103115CAS No.: 443144-27-2Synonyms: EMD 281014; LY 2422347 hydrochloridePruvanserin hydrochloride (EMD 281014) is a selective serotonin 5-HT2A receptor antagonist with IC50 values of 0.35 nM and 1 nM for human and rat 5-HT2A receptors. Pruvanserin (hydrochloride) can be used for the research of schizophrenia.
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SB-247853
0 ImagesCat. No.: HY-19297CAS No.: 200711-10-0SB-247853 is a highly specific 5-HT2c receptor antagonist. SB-247853 induces orthostatic intolerance during head-up tilting. SB-247853 can be used in the research of cardiovascular diseases.
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Dolasetron-d5
0 ImagesCat. No.: HY-B0750S1Synonyms: MDL-73147-d5Dolasetron (MDL-73147)-d5 is deuterated labeled Dolasetron (HY-B0750). Dolasetron is a serotonin 5-HT3 receptor antagonist. Dolasetron acts as an antiemetics agent and can be used for the research of chemotherapy-induced nausea and vomiting in cancer.
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PUC-10
0 ImagesCat. No.: HY-172678CAS No.: 2064126-76-5PUC-10 is a 5-HT6 receptor antagonist with a Ki of 14.6 nM and an IC50 of 32 nM. In silico predictions suggest that PUC-10 is orally active and can cross the blood-brain barrier. PUC-10 can induce autophagy in SH-SY5Y cells by inhibiting the mTOR pathway. PUC-10 can be used in the research of neurological disorders.
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Nexopamil
0 ImagesNexopamil is a calcium antagonist of Ca2+ channel, 5HT2, 5HT1A, 5HT1C and dopamine D2 receptors. Nexopamil exhibits vasodilatory, cardioprotective, and platelet aggregation inhibiting effects. Nexopamil can be used for researches of stable or unstable angina and possibly of peripheral arterial occlusive disease.
