Selected C8 two-chain linkers enhance the adenosine A₁/A_2A receptor affinity and selectivity of caffeine

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• 作者：M.M. van der Walt^a ; ^{dalenevanderwalt@gmail.com} ; ^{13035134@nwu.ac.za} ; G. Terre'Blanche^a ; ^b
• 关键词：Caffeine ; Adenosine A2A receptor antagonist ; Adenosine A1 receptor antagonist ; 1 ; 3 ; 7-trimethylxanthine ; Parkinson's disease
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：652-656
• 全文大小：386 K
• 卷排序：125

文摘

Selected C8 two-chain linkers yield enhanced adenosine receptor affinity. A1 receptor antagonists are considered agents for Parkinson's disease therapy. A2A receptor antagonists are considered agents for Parkinson's disease therapy. Introduction of a para-chloro substitution govern A2A receptor selectivity.