Diimidazo[1,2-c:4′,5′-e]pyrimidines: Adenosine agonist activity demonstrated by microphysiometry

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• 作者：Camp ; David ; Green ; Jennifer M. ; Kaiser ; Sonya M. ; Moni ; Roger W. ; Townsend-Nicholson ; Andrea ; et. al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1998
• 出版时间：March 17, 1998
• 年：1998
• 卷：8
• 期：6
• 页码：691-694
• 全文大小：260 K

文摘

Silicon-based microphysiometry, measuring extracellular acidification rate of cells in culture, demonstrated that a series of diimidazo[1,2-c:4′,5′-e]pyrimidines were agonists at the human adenosine A₁ receptor. 5-amino-7,8-dihydro-3-ribofuranose-8-(R)-(phenyl)-3H-diimidazo[1,2-c:4′,5′-e]pyrimidine (2a) had an EC₅₀ of 100 μM and reached 90 % of the E_max produced by R-PIA.