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本文对包甲素天然品和合成品的缩瞳作用和药效动力学进行比较,证明相同浓度(0.026%)的眼药水天然品家兔滴眼可使瞳孔面积缩小63%,而合成品则仅为29.9%,但排便、流涎等副作用亦相应减轻,药效动力学研究证明天然品和合成品的量—效曲线有相同的斜率和最大收缩效应,但解离常数相差2～3倍,合成品量—效曲线平行右移。以上结果提示:①包甲素合成品是消旋体,可以代替天然品或匹罗卡品用于胃光眼治疗;②包甲素是一个典型的M—胆硷受体完全激动剂;③包甲素及其合成类似物的研究将可进一步阐明M—受体模型和莨菪烷类生物硷的构效关系。
In this paper, the contractile effect and pharmacodynamics of natural and synthetic products of taiyuan are compared. It is proved that eye drops with the same concentration (0.026%) can reduce pupil area by 63%, while synthetic products Only 29.9%. However, side effects such as defecation and salivation were correspondingly alleviated. Pharmacodynamic studies showed that the volume-effect curves of natural products and synthetic products had the same slope and maximum systolic effect, but the dissociation constants differed by 2 to 3 times. The amount of synthetic products - the effect of moving parallel to the right curve. The above results suggest that: (1) Baoganzheng synthetic product is racemic, can replace natural or pilocarpine for the treatment of gastropathy; ② Baoganxin is a typical M-cholinergic receptor agonist; ③ The study of Baoguang and its synthetic analogues will further elucidate the structure-activity relationship between the M-receptor model and tropane alkaloids.