Review Article

PDE10A抑制剂用于中枢神经系统相关疾病的发现进展。第一部分:化学和生物研究综述

卷 20, 期 1, 2019

页: [122 - 143] 页: 22

弟呕挨: 10.2174/1389450119666180808105056

价格: $65

摘要

磷酸二酯酶10A(PDE10A)是水解环-3‘,5’-腺苷单磷酸(CAMP)和环-3‘,5’-鸟苷酸(CGMP)等第二信使分子的双底物酶。通过这一过程,PDE10A控制着哺乳动物大脑和外周组织中的细胞内信号通路。药理、生化和解剖学资料表明,PDE10A介导的第二信使系统的紊乱可能导致中枢神经系统(CNS)功能的损害,包括认知缺陷以及行为、情感处理和运动障碍。本文综述了PDE10A的详细描述和选择性PDE10A抑制剂设计的最新进展。本文还总结了PDE10A抑制剂治疗中枢神经系统相关疾病(如精神分裂症、亨廷顿病和帕金森病)的临床前研究结果。

关键词: PDE10A抑制剂,第二信使系统,SAR研究,中枢神经系统紊乱,罂粟碱相关化合物,异喹啉。

图形摘要

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