四氢原小檗碱同类物与多巴胺D_2受体作用的定量构效关系  

Quantitative StructureActivity Relationships forTetrahydroprotoberberines to Interact with the Dopamine D2 Receptor

作　　者：傅旭春[1,2] 胡永洲[1,2] 周启霆 白东鲁[1,2] 

机构地区：[1]浙江大学药学院 [2]中国科学院上海药物研究所

出　　处：《中国药物化学杂志》1999年第2期111-113,共3页Chinese Journal of Medicinal Chemistry

摘　　要：四氢原小檗碱同类物是一类新型的脑内多巴胺受体阻滞剂．本文用ＦｒｅＷｉｌｓｏｎ法研究了一组四氢原小檗碱同类物与多巴胺Ｄ２受体作用的定量构效关系．结果表明：Ｃ２位上的ＯＨ和Ｃ１２位上的Ｃｌ使四氢原小檗碱同类物与多巴胺Ｄ２受体的亲和力增强，Ｃ１１位上的立体位阻可能使亲和力降低，Ｃ１０位上的取代基可能对亲和力影响不大．Tetrahydroprotoberberines are novel antagonists on dopamine receptors in the brain.In the present paper,we describe the quantitative structureactivity relationships for tetrahydroprotoberberines to interact with the dopamine D2 receptor by the FreeWilson method.The OH group at the position2 and Cl group at the position 12 are beneficial to their affinities with the dopamine D2 receptor.The steric hinder at the positon 11 is unfavourable.Substituents at the position 10 have little effect on the affinities.

关 键 词：四氢原小檗碱 同类物 多巴胺受体 定量构效关系 

分 类 号：R971.94[医药卫生—药品] R962[医药卫生—药学]