Barnes N M, Costall B, Naylor R J, Tattersall F D
Postgraduate School of Studies in Pharmacology, University of Bradford, UK.
J Pharm Pharmacol. 1988 Aug;40(8):586-8. doi: 10.1111/j.2042-7158.1988.tb05312.x.
The 5-HT3 receptor antagonist [3H]zacopride was used to identify 5-HT3 recognition sites in the ferret area postrema. Specific binding was determined by the inclusion of the 5-HT3 receptor antagonist BRL 43694 in the incubation media, and was shown to be much higher in the area postrema than in other brain regions. The increased binding in the area postrema may reflect either a greater number of binding sites, a higher affinity for such sites, or both. The results indicate that 5-HT3 recognition sites are present within the area postrema and may afford an antiemetic site of action for zacopride and other 5-HT3 receptor antagonists.
5-羟色胺3(5-HT3)受体拮抗剂[3H]扎考必利被用于识别雪貂最后区的5-HT3识别位点。通过在孵育培养基中加入5-HT3受体拮抗剂BRL 43694来测定特异性结合,结果显示最后区的特异性结合比其他脑区高得多。最后区结合增加可能反映结合位点数量更多、对这些位点的亲和力更高,或者两者兼而有之。结果表明,5-HT3识别位点存在于最后区内,可能为扎考必利和其他5-HT3受体拮抗剂提供一个止吐作用位点。