神经甾体的药理活性及作用机制  

The Pharmacological Activities and Molecular Mechanisms of Action of Neurosteroids

作　　者：陈宏奎[1] 何玲[1] 刘国卿[1] 季晖[1] 

机构地区：[1]中国药科大学药理学教研室,江苏南京210009

出　　处：《药学进展》2008年第3期115-121,共7页Progress in Pharmaceutical Sciences

基　　金：江苏省博士后科研资助项目(No.0601050B)

摘　　要：综述神经甾体的合成与代谢、药理活性、作用机制及其构效关系。神经甾体是脑中或外周神经系统合成的一些类固醇,在神经发育以及病理生理学过程中起非常重要的作用。有大量证据显示,神经甾体与成人的神经/精神性疾病,包括阿尔茨海默病、精神分裂症、癫痫、情绪紊乱、焦虑症和创伤后精神紧张性障碍等有关。因此,对其作用机制和构效关系的明确认识有助于这些疾病的治疗与相关药物的开发。The pharmacological activity, molecular mechanisms of action and structure-activity relationships of neurosteroids were reviewed in this paper. Neurosteroids which are steroids synthesized by the brain and peripheral nervous system, play a significant role in neurodevelopment and are involved in a wide variety of psychopathological processes. There is accumulating evidence chopathology of some diseases, including Alzheimer disease, schizophrenia, on their role in adult psyseizures, mood disorder, anxiety disorders, post-traumatic stress disorder, and so on. The definite recognition of the pharmacological activity, molecular mechanisms of action and structure-activity relationships of neurosteroids will be helpful for the therapeutic benefit and drug discovery.

关 键 词：神经甾体 构效关系 GABAA受体 激动剂 拮抗剂 

分 类 号：R96[医药卫生—药理学]