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
(576)
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5-HT1 Receptor
(455)
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5-HT2 Receptor
(490)
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5-HT3 Receptor
(35)
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5-HT4 Receptor
(19)
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5-HT5 Receptor
(14)
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5-HT6 Receptor
(86)
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5-HT7 Receptor
(89)
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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 (1774)
Related Products (1774)
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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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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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SB-269970
0 ImagesSB-269970 is a potent, selective and brain-penetrant 5-HT7 receptor antagonist with a pKi of 8.3. SB-269970 exhibits >50-fold selectivity against other 5-HT receptors.
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Alprenolol hydrochloride
0 ImagesSynonyms: (RS)-Alprenolol hydrochloride; dl-Alprenolol hydrochlorideAlprenolol ((RS)-Alprenolol; dl-Alprenolol) hydrochloride is an orally active non-selective β-adrenoceptor antagonist and an antagonist of 5-HT1A and 5-HT1B receptors. Alprenolol hydrochloride is used as an anti-hypertensive, anti-anginal and anti-arrhythmic agent.
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Palonosetron hydrochloride
0 ImagesPalonosetron hydrochloride is a 5-HT3 antagonist primarily used to prevent acute, delayed, and overall chemotherapy-induced nausea and vomiting. In addition, Palonosetron hydrochloride exhibits moderate anti-flavivirus activity and potent anti-Zika virus activity in mammalian cells. Palonosetron hydrochloride also possesses antidepressant activity.
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Thioridazine
0 ImagesThioridazine, an antagonist of the dopamine receptor D2 family proteins, exhibits potent anti-psychotic and anti-anxiety activities. Thioridazine is also a potent inhibitor of PI3K-Akt-mTOR signaling pathways with anti-angiogenic effect. Thioridazine shows antiproliferative and apoptosis induction effects in various types of cancer cells, with specificity on targeting cancer stem cells (CSCs).
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Loxapine
0 ImagesLoxapine is an orally active dopamine inhibitor, 5-HT receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
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Ondansetron hydrochloride
0 ImagesSynonyms: GR 38032 hydrochloride; SN 307 hydrochlorideOndansetron (GR 38032; SN 307) hydrochloride is a highly selective 5-HT3 receptor antagonist with an IC50 value of 103 pM. Ondansetron hydrochloride exerts its antiemetic effect by antagonizing 5-HT receptors located in localized neurons in the peripheral and central nervous systems. Ondansetron hydrochloride can inhibit nausea and vomiting induced by chemotherapy and radiotherapy.
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Trimipramine maleate
0 ImagesTrimipramine maleate is a 5-HT receptor antagonist, with blood-brain barrier permeability. Trimipramine maleate has pKi binding values of 6.39, 8.10, 4.66 for 5-HT1C, 5-HT2 and 5-HT1A, respectively. Trimipramine maleate is also a potent and selective inhibitor targeting human noradrenaline (hNAT), serotonin (hSERT) and organic cation transporters (hOCT1, hOCT2) with IC50 values of 4.99 μM, 2.11 μM, 3.72 μM, 8.00 μM, respectively. Trimipramine maleate has vascular activity and anxiolytic efficacy.
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Trazodone hydrochloride
0 ImagesSynonyms: AF-1161Trazodone hydrochloride (AF-1161) is a triazolopyridine derivative that belongs to the class of serotonin receptor antagonists and reuptake inhibitors (SARIs). Trazodone hydrochloride has anti-depressant and anti-insomnious activity. Trazodone hydrochloride exerts antagonistic properties against a1- and a2-adrenergic receptors and histamine H1 receptors, with minimal anticholinergic effects.
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Granisetron Hydrochloride
0 ImagesSynonyms: BRL 43694AGranisetron (Hydrochloride) (BRL 43694A) is a serotonin 5-HT3 receptor antagonist used as an antiemetic to treat nausea and vomiting following chemotherapy.
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RS-127445
0 ImagesRS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites.
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S1RA hydrochloride
0 ImagesSynonyms: E-52862 hydrochlorideS1RA (E-52862) hydrochloride is an orally active and selective sigma-1 receptor (σ1R) antagonist with a Ki value of 17 nM. S1RA hydrochloride shows good selectivity against σ2R (Ki >1000 nM). S1RA hydrochloride is a human 5-HT2B receptor antagonist with an IC50 value of 4.7 μM. S1RA hydrochloride inhibits neuropathic pain and activity-induced spinal sensitization.
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Hordenine
0 ImagesHordenine (Ordenina; Peyocactine) is a multifunctional alkaloid with oral activity and blood-brain barrier penetration. Hordenine inhibits LPS-induced phosphorylation of p38, JNK, ERK1/2, p65, IκB, and AKT, prevents p65 nuclear translocation, and suppresses inflammatory cytokines and mediators. Hordenine promotes M2 macrophage polarization, restores blood-milk barrier integrity, alleviates oxidative stress by reducing ROS and MDA, and attenuates LPS-induced lung injury and pulmonary edema. Hordenine inhibits cAMP production, CREB phosphorylation, and MITF expression, thereby suppressing melanin synthesis in melanocytes and reconstructed epidermis. Hordenine activates the Wnt/β-catenin signaling pathway, promotes dermal papilla cell proliferation and hair shaft elongation, and accelerates hair regeneration. Hordenine activates DRD2, acts as a D3R partial agonist, α2A-AR full agonist, and 5-HT2A-R antagonist, and inhibits SERT and DAT. Hordenine inhibits α-synuclein accumulation and ameliorates motor deficits in Parkinson's disease models. Hordenine limits alcohol intake, reduces relapse drinking behavior, and modulates alcohol-induced conditioned place preference. Hordenine 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.
