郑璐,侯景轩,郝帅帅,吴庆昆.化学通报,2022,85(3):303-308.
GPR52---治疗神经系统疾病的新靶点
GPR52---A New Target for CNS Diseases
投稿时间:2021-07-05  修订日期:2021-09-13
DOI:
中文关键词:  GPR52,G蛋白偶联受体,精分,亨廷顿舞蹈症,激动剂,反向激动剂
英文关键词:GPR52, G protein coupled receptor, schizophrenia, Huntington
基金项目:
作者单位E-mail
郑璐 江苏海洋大学 药学院 zhel-123@163.com 
侯景轩 江苏海洋大学 药学院  
郝帅帅 江苏海洋大学 药学院  
吴庆昆* 江苏海洋大学 药学院 qingkunwuchem@163.com 
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中文摘要:
      GPR52是G蛋白偶联受体家族的一员,它的内源性配体至今仍未发现。但其在大脑纹状体中高度表达,能够抑制多巴胺D2受体并通过促进神经细胞中cAMP的积累激活多巴胺D1受体和NMDA受体,成为治疗精神分裂症的潜在靶点。同时GPR52受体反向激动剂被证明不仅可以降低mHTT的水平而且能够治疗小鼠模型中的亨廷顿病相关症状。
英文摘要:
      GPR52 is a member of the G protein-coupled receptor family, and its endogenous ligand has not been found so far. However, it is highly expressed in the striatum species of the brain, and can inhibit the dopamine D2 receptor and activate the dopamine D1 receptor and NMDA receptor by promoting the cAMP level of nerve cells, thus becoming a potential target for the treatment of spermatosis. Meanwhile, GPR52 receptor inverse agonists have been shown to not only reduce mHTT levels but also treat symptoms associated with Huntington"s disease in a mouse model.
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