Adenosine A2A Receptor Antagonists and Parkinson's Disease

被引：90

作者：

Shook, Brian C. ^{[1
]}

Jackson, Paul F. ^{[1
]}

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev LLC, Spring House, PA 19477 USA

来源：

ACS CHEMICAL NEUROSCIENCE | 2011年 / 2卷 / 10期

关键词：

Adenosine; A(2A) receptor antagonist; A(1) receptor antagonist; Parkinson's disease; catalepsy; 6-OHDA; MPTP; PHARMACOLOGICAL CHARACTERIZATION; HUMAN BRAIN; L-DOPA; POTENT; DESIGN; OPTIMIZATION; MODELS; A(1); RAT; DYSKINESIA;

D O I：

10.1021/cn2000537

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：

This Review summarizes and updates the work on adenosine A(2)A receptor antagonists for Parkinson's disease from 2006 to the present. There have been numerous publications, patent applications, and press releases within this time frame that highlight new medicinal chemistry approaches to this attractive and promising target to treat Parkinson's disease. The Review is broken down by scaffold type and will discuss the efforts to optimize particular scaffolds for activity, pharmacokinetics, and other drug discovery parameters. The majority of approaches focus on preparing selective A2A antagonists, but a few approaches to dual A(2A)/A(1) antagonists will also be highlighted. The in vivo profiles of compounds will be highlighted and discussed to compare activities across different chemical series. A clinical report and update will be given on compounds that have entered clinical trials.

引用

页码：555 / 567

页数：13

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