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Request The Product List of5-HT Receptor 5-HT 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.

Cat. No. Product Name CAS No. Information
GY03985

Eptapirone

179756-58-2

A potent, selective 5-HT1A receptor agonist with Ki of 4.8 nM, pKi of 8.33; shows ≥shows 100-fold higher affinity for the other serotonin receptor subtypes, and has no detectable antidopaminergic activity and antihistaminergic activity; decreases the forskolin-induced increase in AMP in HeLa cells expressing human 5-HT1A receptors; produces anxiolytic- and antidepressant-like effects in animal models.

GY07028

NBUMP

1348755-27-0

NBUMP is a potent, highly selective 5-HT1A receptor partial agonist with Ki of 0.1 nM, displays 460- and 260-fold selectivity for 5-HT1A over the α1-adrenergic and D2 receptors, respectively.

GY07027

Minesapride

1184662-54-1

Minesapride (DSP-6952) is a novel potent, selective, orally active 5-HT4 receptor partial agonist with Ki of 50-100 nM for human 5-HT4a/4b/4c; enhances gastric motility and causes colonic giant migrating contractions (GMCs) associated with defecation in conscious dogs, having ED50 value for inducing GMCs of 1.56 mg/kg; rapidly increases fecal wet weight without increasing fluid content in mice (1-10 mg/kg, p.o.).

GY06804

Pruvanserin hydrochloride

443144-27-2

EMD-281014 hydrochloride ((Pruvanserin, LSN2411347, LY-2422347)) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels; significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test; reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset.

GY06803

Pruvanserin

443144-26-1

EMD-281014 ((Pruvanserin, LSN2411347, LY-2422347)) is a potent, highly selective 5-HT2A antagonist with Ki of 0.87 nM, displays little to no affinity for 5-HT2C receptors (Ki=557 nM), human D2 receptors and IKr channels; significantly increases swimming and decreases immobility in male congenital learned helpless rats in the forced swim test; reduces dyskinesia and psychosis in the l-DOPA-treated parkinsonian marmoset.

GY04044

BRL54443

57477-39-1

BRL54443 is a potent, releative selective 5-HT1E/1F agonist with Ki of 2/1 nM, respectively; shows low affinity for other receptors 5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM); selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production with IC50 of 14 nM in DG membranes; significantly reduces formalin-induced flinching in rats.

GY04015

Eletriptan hydrobromide

177834-92-3

Eletriptan (UK 116044) is a potent, selective, and orally active 5-HT1B/1D receptor agonist; significantly increases occluded wedge pressure and mean pulmonary artery pressure in vivo, with no significant coronary artery constriction, and obstructive coronary artery disease; displays antimigraine activity.

GY03571

Nelotanserin

839713-36-9

A potent, selective 5-HT2A inverse agonist with pKi of 9.2; displays >30- and 5000-fold selectivity compared with 5-HT2C and 5-HT2B receptors; prevents DOI-induced hypolocomotion and increases sleep consolidation; orally active.

GY05046

Ziprasidone hydrochloride

122883-93-6

A full antagonist of D2 and 5-HT2A receptors with Ki of 6.8 and 0.6 nM, respectively; also is a partial agonist of 5-HT1A, and a partial antagonist of 5-HT2C and 5-HT1D receptors; exhibits potent antipsychotic activity in vivo.

GY05045

Ziprasidone hydrochloride monohydrate

138982-67-9

A full antagonist of D2 and 5-HT2A receptors with Ki of 6.8 and 0.6 nM, respectively; also is a partial agonist of 5-HT1A, and a partial antagonist of 5-HT2C and 5-HT1D receptors; exhibits potent antipsychotic activity in vivo.

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