一系列毒蕈碱样药物中的定量构效关系
QSAR in a series of muscarinic agents.
作者信息
Pratesi P, Villa L, Ferri V, De Micheli C, Grana E, Grieco C, Silipo C, Vittoria A
出版信息
Farmaco Sci. 1979 Aug;34(8):657-65.
The results of a pharmacological investigation on a series of 3-substituted benzyltrimethylammonium salts possessing muscarinic activity are reported. Correlative analysis shows that the pharmacodynamic activity is a function of the hydrophobic-lipophilic and steric parameters associated with the substituents. In particular, it is revealed that a lipophilic pocket of limited size is present in the muscarinic receptor at an optimal distance from the electron--rich site with which the cationic termination interacts.
报道了对一系列具有毒蕈碱活性的3-取代苄基三甲基铵盐的药理学研究结果。相关分析表明，药效学活性是与取代基相关的疏水-亲脂性和空间参数的函数。特别地，结果显示在毒蕈碱受体中存在一个尺寸有限的亲脂性口袋，其与阳离子末端相互作用的富电子位点具有最佳距离。
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