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新型抗精神病药物的发现:多巴胺和血清素受体调制作用。

Recent developments in the discovery of novel antipsychotic agents modualating dopamine and serotonin receptors.

机构信息

Department of Medicinal Chemistry, Key Laboratory of Chemical Biology (Ministry of Education), School of Pharmaceutical Sciences, Shandong University, 44 West Culture Road, Jinan 250012, PR China.

出版信息

Curr Drug Targets. 2013 Jul;14(8):899-918. doi: 10.2174/13894501113149990007.

DOI:10.2174/13894501113149990007
PMID:23701299
Abstract

Currently, schizophrenia, as a serious psychiatric disorder, continues affecting the quality of life in the psychotics. This disease is often debilitating and chronic, showing broad symptoms at one end by hallucinations, delusions, thought disorder and the other end by affective flattening, catatonia, social isolation. In order to combat this disease, many antipsychotic drugs have been developed and introduced into clinical practice in the past half century. However, only a small minority of them can treat effectively schizophrenia without side effects. In view of this situation, high attention has been given to the exploration of desired antipsychotic agents influential especially through the modulation of dopamine and serotonin receptors with substantial strides made in recent years, leading to the discovery of many novel chemical entities with intriguing profiles. In this review, we summarize novel structural antipsychotics in development and discuss the future direction of ideal antipsychotic drug candiates. In particular, the promising atypical antipsychotic profiles of new molecules and the inspirations for their design are highlighted.

摘要

目前,精神分裂症作为一种严重的精神疾病,持续影响着精神病患者的生活质量。这种疾病通常使人衰弱和慢性,在一端表现出幻觉、妄想、思维障碍等广泛的症状,在另一端表现出情感迟钝、木僵、社交隔离等症状。为了治疗这种疾病,过去半个世纪已经开发并引入了许多抗精神病药物进入临床实践。然而,只有少数药物可以有效治疗精神分裂症而没有副作用。鉴于这种情况,人们高度关注探索理想的抗精神病药物,特别是通过调节多巴胺和血清素受体,近年来取得了实质性进展,发现了许多具有有趣特征的新型化学实体。在这篇综述中,我们总结了正在开发的新型结构的抗精神病药物,并讨论了理想抗精神病候选药物的未来方向。特别强调了新分子的有前途的非典型抗精神病特征及其设计灵感。

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