Uses
BGC 20-761, is a selective high affinity 5-HT6 antagonist (Ki = 20 nM). that has shown to enhance memory consolidation in a rat model. It reverses he amnesic effects of Scopolamine (S200000).
Biological Activity
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.
in vivo
BGC20-761 enhances memory consolidation and reverses scopolamine-induced memory deficit in social and visuospatial memory tasks through a 5-HT6 receptor-mediated mechanism. BGC20-761 (2.5 mg/kg, 5 mg/kg and 10 mg/kg; i.p.) alone has no effect on social recognition in young rats, however, at doses of 5 mg/kg and 10 mg/kg i.p, BGC20-761 dose-dependently reverses a deficit of social recognition induced by Scopolamine (0.4 mg/kg i.p.)[1].
| Animal Model: | Forty-two male 8-week-old Longe Evans rats and 12 male four-week-old SpragueeDawley rats[1] |
| Dosage: | 2.5 mg/kg, 5 mg/kg and 10 mg/kg |
| Administration: | Administered (i.p.) immediately after the training session for the social recognition test |
| Result: | Administered alone did not show any difference in social recognition as compared to saline treated control animals.
However, 5 mg/kg and 10 mg/kg reversed a Scopolamine induced deficit in social recognition. |
IC 50
Human 5-HT6 Receptor: 20 nM (Ki); Human 5-HT2A Receptor: 69 nM (Ki); Human D2 Receptor: 140 nM (Ki)
References
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.
