摘要
目的:6β-乙酰氧基去甲托烷(6β-AN)是新合成的外消旋莨菪烷衍生物,实验表明为M受体激动剂。本课题从离体水平,对其化学拆分后的左旋体(l-6β-AN)对家兔虹膜上M胆碱受体及其亚型选择性作用进行研究,来阐明其作用机制。方法:制备离体虹膜标本,用累积浓度法制作量效关系曲线。结果:l-6β-AN对离体虹膜括约肌呈现明显的浓度依赖性收缩,用选择性M受体拮抗剂研究表明,与虹膜收缩有关的受体亚型为M3受体。结论:l-6β-AN致虹膜收缩主要是激动虹膜上M受体所致,并且对虹膜上M3受体选择性较强。
Objective :6β-Acetoxy nortropane(6β-AN) is a newly synthesized derivative of nortropane. Animal tests have shown that it is an agonist of muscarinic cholinergic receptor. This study, which was conducted in vitro, was to investigate the selective effects of 1 -6β-AN on the muscarinic cholinergic receptor and its subtypes on irises of rabbits, and to illuminated the mechanism of its action. Method:To prepare the isolated iris sanyle and to make dose - effect relationship curve in a concentration - accumulated manner. Results: The pharmacodynamic test on isolated irises of rabbits showed that 1 - 6β- AN caused a concentration - dependent contraction. The Study with selective M receptor antagonists showed that the M receptor subtype associated with iris contraction was M3 receptor. Conclusion:The isolated iris contraction caueed ty 1 - 6β-AN was due to activaton of M receptor on the iris. 1- 6β-AN had a relatively strong selective effect on M3 subtype receptors on iris.
出处
《牡丹江医学院学报》
2006年第5期10-12,共3页
Journal of Mudanjiang Medical University
关键词
去甲托烷
M胆碱受体
受体亚型
拮抗剂
离体虹膜
nortropane
Muscarinic cholinergic receptor
subtypes
antagonists
isolated iris