包甲素合成类似物的过筛试验  

A Screening Test for Boajiasu Derivatives

作　　者：冯菊妹[1] 张佩瑾[1] 俞霭瑶[1] 孙琛[1] 

机构地区：[1]上海第二医科大学药理学教研室

出　　处：《上海第二医科大学学报》1990年第4期324-326,共3页Acta Universitatis Medicinalis Secondae Shanghai

摘　　要：本文采用豚鼠离体纵长肌累积剂量-效应曲线法,求解离常数(KD)及最大效应(Emax)值,以氨甲酰胆碱为标准药,对14个莨菪烷类化合物进行比较,结果表明:6β-乙酰氧基去甲莨菪烷,3α-对甲苯甲酰氧基-6β-乙酰氧基莨菪烷及3α,6β-二乙酰氧基莨菪烷三化合物有明显的M受体激动作用。其构-效关系提示:6β-乙酰氧基是M激动作用的关健结构,N位上的CH_3能削弱这一作用。The KD and Emax of 14 Boajiasu derivatives (Tropanes) were compared with typical M-cholinoceptor agonist carbachol by using cumulative dose-response curve method on isolated ileum longitudinal muscle of guine pig.The results proved that 6β-acetoxy nortropane, 3α-paramethyl benzoyloxy-6β-acetoxy tropane, and 3α, 6β-acetoxy tropane possess significant M-cholineceptor agonistic action. The preliminary study on their structure-activity relationship suggests that 6β-acetoxy group is the basal structure for M-agonistic activity, while N-CH_3 would weaken the activity.

关 键 词：莨菪烷类 包甲素 过筛试验 

分 类 号：R965.1[医药卫生—药理学]