1, 3-Dialkyl-8-(p-sulfophenyl) xanthines: potent water-soluble antagonists for A1-and A2-adenosine receptors

…, W Padgett, MT Shamim, P Butts-Lamb…

Index: Daly, J.W.; Padgett, W.; Shamim, M.T.; Butts-Lamb, P.; Waters, J. Journal of Medicinal Chemistry, 1985 , vol. 28, # 4 p. 487 - 492

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Citation Number: 238

Abstract

A series of & (substituted phenyl) derivatives of theophylline and other 1, 3-diakylxanthmes were evaluated for potency and selectivity as antagonists at A,-and A2-adenosine receptors in brain tissue. Theophylline has a similar potency (Ki= 14~ LM) at both A, and A2 receptors. 8-Phenyltheophylline is 25-35-fold more potent as an adenosine receptor antagonist than theophylline, while 8-phenylcaffeine is only 2-3-fold more potent than caffeine. A p- ...