2-Alkynyl derivatives of adenosine and adenosine-5'-N-ethyluronamide as selective agonists at A2 adenosine receptors

G Cristalli, A Eleuteri, S Vittori, R Volpini…

文献索引：Cristalli; Eleuteri; Vittori; Volpini; Lohse; Klotz Journal of Medicinal Chemistry, 1992 , vol. 35, # 13 p. 2363 - 2368

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被引用次数: 127

摘要

In the search for more selective A2-receptor agonists and on the basis that appropriate substitution at C2 is known to impart selectivity for A2 receptors, 2-alkynyladenosines 2a-d were resynthesized and evaluated in radioligand binding, adenylate cyclase, and platelet aggregation studies. Binding of [3H] NECA to Az receptors of rat striatal membranes was inhibited by compounds 2a-d with Ki values ranging from 2.8 to 16.4 nM. 2- ...