BGC 20-761 是一种选择性 5-HT6 和多巴胺受体拮抗剂（人受体 Ki 值：5-HT6 (20 nM)、5-HT2A (69 nM)、D2 (140 nM)）。
BGC20-761 is a selective and high affinity antagonist of 5-HTC.
The 5-HT6 receptor, a G protein-coupled receptor (GPCR), is a subtype of 5-HT receptor which binds the endogenous neurotransmitter serotonin (5-hydroxytryptamine, 5-HT). This protein is expressed almost exclusively in the brain and mediates excitatory neurotransmission.
In cellular level, BGC20-761 (5-methoxy-2-phenyl-N,N-dimethyltryptamine) was shown to selectively blocked 5-HTC.
BGC20-761 was used to study the difference in drug- induced effects in memory consolidation in young and mature rats and human. In young mice, BGC20-761 treatment at doses of 5 mg/kg and 10 mg/kg i.p, dose-dependently reversed a deficit of social recognition induced by scopolamine, an anticholinergic drug that impairs memory at dosage of 0.4 mg/kg i.p. In mature rats (6 months), recognition of the novel object was improved following administration of BGC20-761. The difference in effects of BGC20-761 in young vs. mature rats may reflect the status of memory consolidation in these different age ranges 1.
Reference:
1.? Mitchell ES, Hoplight BJ, Lear SP, et al. BGC20-761, a novel tryptamine analog, enhances memory consolidation and reverses scopolamine-induced memory deficit in social and visuospatial memory tasks through a 5-HT6 receptor-mediated mechanism. Neuropharmacology. 2006;50(4):412-420.
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