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常见的神经系统疾病如药物成瘾及其导致的神经毒性、神经精神疾病、神经退行性疾病等,严重影响人类健康与正常生活。而临床上现有的相关治疗药物往往会导致锥体外系反应等副作用,且用药后治疗不够彻底,疾病易复发,因此,开发新靶点及新型有效、安全的相关治疗药物,迫在眉睫。Sigma-1受体是一种受体型分子伴侣,参与多种神经传导系统的调节,可与多种精神类药物结合,有望成为神经系统调节药物的重要靶点。研究发现,有些小分子配体对Sigma-1受体具有良好的亲和力,在药物成瘾、精神分裂症、抑郁症、阿尔茨海默病等疾病中显示出较好疗效。对Sigma-1受体的药理学作用以及相关小分子配体药物的研发作一综述。
Common neurological diseases such as drug addiction and its resulting neurotoxicity, neuropsychiatric disorders, neurodegenerative diseases, seriously affect human health and normal life. However, the existing clinically relevant therapeutic drugs often cause side effects such as extrapyramidal reactions, and the treatment is not thorough enough after treatment and the diseases are easy to recur. Therefore, it is imminent to develop new targets and new effective and safe related therapeutic drugs. Sigma-1 receptor is a receptor chaperone involved in the regulation of a variety of nerve conduction system, with a variety of psychotropic drugs, is expected to become an important target of the nervous system regulating drugs. The study found that some small molecule ligands have good affinity for Sigma-1 receptor, and show good efficacy in diseases such as drug addiction, schizophrenia, depression and Alzheimer’s disease. The pharmacological effects of Sigma-1 receptor and the development of related small molecule ligand drugs are reviewed.