【摘要】 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。更多还原

【Abstract】 Common nervous system disorders, such as drug addiction and related neurotoxicity, neuropsychiatric disorders, neurodegenerative diseases, ect., affect seriously human health and daily life. However, current related therapies in the clinlic are often associated with adverse effects such as extrapyramidal side effects(EPS) and with inadequate treatment and disease recurrence. Thus, there still remains an urgent unmet need for new related therapeutic targets and more effective and safer agents. As a receptor chaperon involved in the regulation of multiple neural signal transmission systems, Sigma-1 receptor can bind with diverse antipsychotic drugs and become a promising target for novel nervous system drugs. Several smallmolecule ligands have been identified with excellent affinity to Sigma-1 receptor and displayed good efficacy in the treatment of drug addiction, schizophrenia, depression, Alzheimer’s disease and so on. In this article, the pharmacological effects of Sigma-1 receptor and the development of its small-molecule ligands as drugs were reviewed.更多还原