CAJ | 학술논문

利用Hansch方法，研究了37种benztropine类化合物diphenylmethoxy部位苯环取代基结构与其活性的定量关系.结果表明：苯环取代基的电性和体积等均是影响该类化合物与多巴胺转运蛋白亲和力的重要因素.所得到的benztropine类化合物diphenylmethoxy部位取代基的综合结构效应，对进一步研究该部位与多巴胺转运蛋白相互作用的电性和立体性质及设计新的多巴胺转运蛋白配体具有指导意义.
이용Hansch방법，연구료37충benztropine류화합물diphenylmethoxy부위분배취대기결구여기활성적정량관계.결과표명：분배취대기적전성화체적등균시영향해류화합물여다파알전운단백친화력적중요인소.소득도적benztropine류화합물diphenylmethoxy부위취대기적종합결구효응，대진일보연구해부위여다파알전운단백상호작용적전성화입체성질급설계신적다파알전운단백배체구유지도의의.
The effect of the aromatic substituents in the diphenylmethoxy ofbenztropine analogs on the affinity for the dopamine transporter is studied using Hansch method. QSAR is found by stepwise and bachward methods of SPSS program. It is demonstrated that the binding affinity is a function of the following parameters: ∑σp(∑R，∑F), Rm2 and Rm4. It is shown that both steric factors and electronic components of substituents of diphenylmethoxy are significant as to the binding affinity at the dopamine transporter. The results may be useful in understanding the interaction of dopamine transporter with benztropine analogs and in designing new benztropine ligands as molecular probes for the dopamine transporter