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作 者:杨飞瀑 何洋[1] 王震[1] 王瑜[1] 蒋翔锐[1] 沈敬山[1]
机构地区:[1]中国科学院受体结构与功能重点实验室,上海药物研究所,上海201203 [2]中国科学院大学,北京100049
出 处:《药学学报》2016年第12期1809-1821,共13页Acta Pharmaceutica Sinica
基 金:上海市科委基金资助项目(Y411161017)
摘 要:流行病学调查表明世界范围内约8‰人患有精神分裂症。目前用于临床的抗精神分裂症药物主要以第二代、第三代抗精神病药为主,该类药物普遍具有D_2受体/5-HT_(2A)受体拮抗作用,对阳性和阴性症状都有效,但是对认知功能障碍的治疗尚不理想,并且往往伴随着心血管和代谢方面的不良反应。为了提高疗效及降低不良反应,近年来科研人员针对其他靶点如D_3受体、谷氨酸受体、PDE10A和H_3受体等抗精神分裂症药物研发开展了较多探索,本文对其进行了系统综述。Epidemiology indicates that schizophrenia affects approximately 8‰ of the world's population. The atypical(second and third generation) antipsychotics generally endowed with D2/5-HT2A receptors antagonism properties are commonly used as first-line drugs for the treatment of schizophrenia presently. They have been proven effective in the treatment of positive and negative symptoms of schizophrenia, but they are largely ineffective in the treatment of cognitive deficit. Moreover, the atypical antipsychotics are usually associated with cardiovascular and metabolic side effects such as QT prolongation and weight gain. To develop more potent antipsychotics with fewer side effects, more targets have been identified such as D3, glutamate, H3 receptors and PDE10A in recent years. Herein, the research progress of antipsychotics is reviewed.
关 键 词:抗精神分裂症药物 D2受体/5-HT2A受体 阳性症状 阴性症状 认知功能障碍
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