摘要
利用Ｈａｎｓｃｈ方法，研究了具有２－毗咯烷基侧链的苯酰胺类化合物的苯环取代基结构与其活性的定量关系．结果表明：苯环Ｒ３位取代基的脂溶性、电性，Ｒ５位取代基的共振效应等均是影响化合物与多巴胺Ｄ２受体亲和力的因素．所得到的取代基的综合结构效应对阐明Ｄ２受体－配体的相互作用机制及设计新的配体具有指导意义．
The influence of the aromatic substituents in the 2, 3 and 5 positions ofbenzamides with 2-pyrmlidinylmethyl side chains on the affinity for the [3H] spiperone binding site is studied. QSAR is found betWeen -logIc50 values and different sets of parameters, i.e.π3, π3, R5 R5 and σm(3+5) by multiple regression calCUlations with SPSS program it isdemonstlated that the binding affinity is affected not only by the lipophilicity and electronicproperties of the 3- substituent but also by asonance effect of the 5- substituent. The resultsmay be useful in understanding the interaction of D2 receptor with ligands and designing newbenzamides dopamine D2 receptor ligands.
出处
《北京师范大学学报（自然科学版）》
CAS
CSCD
北大核心
1999年第4期494-499,共6页
Journal of Beijing Normal University(Natural Science)
基金
国家自然科学基金!29731020
关键词
多巴胺
D2受体显像剂
中枢神经系统
苯酰胺类
Dopamine D2 receptor haging agent
benzamides
the influence of thesubstituents
drug design
