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
(454)
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5-HT2 Receptor
(489)
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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
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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 (1770)
Related Products (1770)
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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-200646A
0 ImagesSB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
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Agomelatine hydrochloride
0 ImagesSynonyms: S-20098 hydrochlorideAgomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
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Idalopirdine hydrochloride
0 ImagesSynonyms: Lu AE58054 hydrochlorideIdalopirdine hydrochloride (Lu AE58054 hydrochloride) is a potent, selective 5-HT6 receptor antagonist with a Ki value of 0.83 nM. Idalopirdine hydrochloride may be used in studies of Alzheimer's disease and schizophrenia, among other related disorders.
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Eplivanserin (mixture)
0 ImagesSynonyms: SR-46349 (mixture)Eplivanserin mixture (SR-46349 mixture) is a selective serotonin reuptake inhibitor and a 5-HT2A receptor antagonist, extracted from patent WO 2005/002578 A1.
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Melperone
0 ImagesMelperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
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Bemesetron
0 ImagesSynonyms: MDL 72222Bemesetron (MDL 72222) is a selective 5-HT3 receptor antagonist with an IC50 of 0.33 nM. Neuroprotective effect.
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Cyanopindolol
0 ImagesCyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively).
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RS 23597-190
0 ImagesSynonyms: EP-A-501322
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Pizotifen malate
0 ImagesPizotifen malate (Pizotyline malate) is a 5-HT2 receptor antagonist. Pizotifen malate inhibits the Wnt/β-catenin-EMT signaling pathway and induces mitochondria-mediated Apoptosis. Pizotifen malate causes transient ERK1/2 phosphorylation and restores ATP. Pizotifen malate blocks Serotonin (HY-B1473A)-mediated platelet activation, inhibits Serotonin-enhanced ADP-induced platelet aggregation, and prolongs carotid artery occlusion and tail bleeding time. Pizotifen malate exhibits anticancer activity against gastric cancer and colon cancer. Pizotifen malate exerts neuroprotective effects in the striatum of R6/2 mice. Pizotifen malate can be used for research on gastric cancer, colon cancer, Huntington's disease, metastasis, and thromboembolic diseases.
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Eplivanserin hemifumarate
0 ImagesSynonyms: SR-46349 hemifumarate; SR 46349BEplivanserin (SR-46349) hemifumarate is a potent, selective and orally active 5-HT2A receptor antagonist, with an IC50 of 5.8 nM in rat cortical membrane, and a Kd of 1.14 nM. Eplivanserin hemifumarate displays >20-fold selectivity more selective for 5-HT2A than 5-HT2B and 5-HT2C.
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Cinanserin hydrochloride
0 ImagesCinanserin hydrochloride (SQ 10643) is a potent, selective and highly affinity 5-HT2 receptor antagonist with a Ki of 41 nM. Cinanserin hydrochloride has a much higher binding affinity for the 5-HT2 than for the 5-HT1 receptor (Ki of 3500 nM). Cinanserin is also an inhibitor of 3C-like proteinase of severe acute respiratory syndrome coronavirus and strongly reduces virus replication in vitro.
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LY310762
0 ImagesLY310762 is a selective 5-HT1D receptor antagonist with a Ki value of 249 nM for the guinea pig receptor. LY310762 blocks presynaptic 5-HT1D autoreceptors and enhances potassium-stimulated [3H]5-HT outflow from guinea pig cortical slices. LY310762 abolishes the inhibitory effect of 5-CT (HY-135555)/L-694,247 (HY-101208) on sympathetic nerve-induced renal vasoconstriction mediated by prejunctional 5-HT1D receptors. LY310762 potentiates the increase in extracellular 5-HT concentration induced by Fluoxetine (HY-B0102). LY310762 is used in research related to depression and diabetic nephropathy.
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Cyamemazine
0 ImagesCyamemazine is a neuroleptic agent that contains the phenothiazine chromophore. Cyamemazine is often used as an anxiolytic. Cyamemazine is a potent 5-HT3 (Ki of 12 nM), 5-HT2A (Ki = 1.5 nM) and 5-HT2C (Ki of 75 nM) receptors antagonist with antipsychotic activity.
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Pirenperone
0 ImagesSynonyms: R 47465Pirenperone (R 47465) is a 5-HT2 serotonin receptor antagonist. Pirenperone exhibits modest anxiolytic activity.
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SB399885
0 ImagesSB399885 is a potent, selective, brain penetrant and orally active 5-HT6 receptor antagonist with pKi values 9.11 and 9.02 for human recombinant and native 5-HT6 receptors, respectively. SB399885 has cognitive enhancing properties.
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Indophagolin
0 ImagesIndophagolin is a potent, indoline-containing autophagy inhibitor (IC50=140 nM). Indophagolin antagonizes the purinergic receptor P2X4 as well as P2X1 and P2X3 with IC50s of 2.71, 2.40 and 3.49 μM, respectively. Indophagolin also antagonizes the Gq-protein-coupled P2Y4, P2Y6, and P2Y11 receptors (IC50s =3.4~15.4 μM). Indophagolin has a strong antagonistic effect on serotonin receptor 5-HT6 (IC50=1.0 μM) and a moderate effect on receptors 5-HT1B, 5-HT2B, 5-HT4e, and 5-HT7.
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Asimilobine
0 ImagesAsimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity.
