Structure-activity relationships of N6-benzyladenosine-5'-uronamides as A3-selective adenosine agonists

C Gallo-Rodriguez, X Ji, N Melman…

Index: Gallo-Rodriguez, Carola; Ji, Xiao-duo; Melman, Neli; Siegman, Barry D.; Sanders, Lawrence H.; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 5 p. 636 - 646

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Citation Number: 226

Abstract

Methyl-N6-(3-iodobenzyl) adenosine displayed a Ki value of 1.1 nM at A3 receptors and selectivity versus A1 and Aareceptors of 50-fold. A series of methoxybenzylderivatives showed that a 4-methoxy group best favored A3 selectivity. A 4-sulfobenzyl derivative was a specific ligand at A3 receptors of moderate potency. An aryl amino derivative was prepared as a probe for radioiodination and receptor cross-linking.