Kwatra M M, Leung E, Hosey M M, Green R D
J Med Chem. 1987 May;30(5):954-6. doi: 10.1021/jm00388a039.
A number of N6-phenyladenosines with various substitutions on the phenyl ring have been synthesized and tested for their affinities toward brain A1 and A2 adenosine receptors. Compounds with meta substituents, such as (m-hydroxy- and m-iodophenyl)adenosine, were found to have high A1 selectivity. Meta substitution caused a selective decrease in the affinity of these compounds for A2 receptors. The results suggest that, in contrast to what is commonly held, certain N6-substituents have pronounced effects on affinity for brain A2 adenosine receptors. Thus, brain A2 receptors may have a well-defined region that recognizes N6-substitutions.
已经合成了一系列在苯环上具有各种取代基的N6-苯基腺苷，并测试了它们对脑A1和A2腺苷受体的亲和力。发现具有间位取代基的化合物，如（间羟基和间碘苯基）腺苷，具有高A1选择性。间位取代导致这些化合物对A2受体的亲和力选择性降低。结果表明，与通常的观点相反，某些N6-取代基对脑A2腺苷受体的亲和力有显著影响。因此，脑A2受体可能有一个明确识别N6-取代基的区域。
