【摘要】 α7 nAChR属于烟碱型乙酰胆碱受体,是由5个α7单体组成的配体门控离子通道。α7 nAChR的配体结合位点主要有两种,即激动剂(拮抗剂)结合位点以及变构调节位点。α7 nAChR是精神分裂症认知障碍以及阿尔茨海默病药物研究的一个重要靶点,现已有多个治疗药物处在临床试验阶段。本文主要综述了α7 nAChR激动剂以及变构调节剂药物的研究进展。更多还原

【Abstract】 α7 nAChR belongs to nicotinic acetylcholine receptor. α7 nAChR is a ligand-gated ion channels which consists of five α7 subunits. A variety of chemotypes could modulate α7 nAChR through interaction at distinct sites on the protein including orthosteric binding sites and PAM binding sites. It has been proved thatα7 nAChR is closely associated with schizophrenia and Alzheimer’s. Several drugs have been in clinical trials. In recent years,various types of novel molecules have been designed and synthesized,which are expected to become a newclass of drugs for schizophrenia and Alzheimer’s.更多还原