Structure-activity relationships at human and rat A2B adenosine receptors of xanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions

SA Kim, MA Marshall, N Melman, HS Kim…

Index: Kim, Soon-Ai; Marshall, Melissa A.; Melman, Neli; Kim, Hak Sung; Mueller, Christa E.; Linden, Joel; Jacobson, Kenneth A. Journal of Medicinal Chemistry, 2002 , vol. 45, # 11 p. 2131 - 2138

Full Text: HTML

Citation Number: 73

Abstract

In the search for improved selective antagonist ligands of the A2B adenosine receptor, which have the potential as antiasthmatic or antidiabetic drugs, we have synthesized and screened a variety of alkylxanthine derivatives substituted at the 1-, 3-, 7-, and 8-positions. Competition for 125I-ABOPX (125I-3-(4-amino-3-iodobenzyl)-8-(phenyl-4-oxyacetate)-1- propylxanthine) binding in membranes of stably transfected HEK-293 cells revealed ...