Development of Adenosine A2A Receptor Antagonists for the Treatment of Parkinson's Disease: A Recent Update and Challenge

被引：51

作者：

Zheng, Jiyue

Zhang, Xiaohu

Zhen, Xuechu

机构：

[1] Soochow Univ, Jiangsu Key Lab Neuropsychiat Dis, Suzhou 215021, Jiangsu, Peoples R China

[2] Soochow Univ, Coll Pharmaceut Sci, Suzhou 215021, Jiangsu, Peoples R China

来源：

ACS CHEMICAL NEUROSCIENCE | 2019年 / 10卷 / 02期

基金：

中国国家自然科学基金;

关键词：

Adenosine receptor; antagonist; Parkinson's disease; GPCR; 5-HT1A DUAL-AGONIST; POTENT; DERIVATIVES; DISCOVERY; DESIGN; AFFINITY; ISTRADEFYLLINE; SELECTIVITY; SCAFFOLD; TARGET;

D O I：

10.1021/acschemneuro.8b00313

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Parkinson's disease (PD) is a neurodegenerative disease with significant unmet medical needs. The current dopamine-centered treatments aim to restore motor functions of patients without slowing the disease progression. Long-term usage of these drugs is associated with diminished efficacy, motor fluctuation, and dyskinesia. Furthermore, the nonmotor features associated with PD such as sleep disorder, pain, and psychiatric symptoms are poorly addressed by the dopaminergic treatments. Adenosine receptor A(2A) antagonists have emerged as potential treatment for PD in the past decade. Here we summarize the recent work (2015-2018) on adenosine receptor A(2A) antagonists and discuss the challenge and opportunity for the treatment of PD.

引用

页码：783 / 791

页数：17

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