Jacobson K A, Yamada N, Kirk K L, Daly J W, Olsson R A
Biochem Biophys Res Commun. 1986 May 14;136(3):1097-102. doi: 10.1016/0006-291x(86)90446-8.
Adenosine analogues substituted at N6 with spacer arms designed for attachment to soluble macromolecules or to solid supports for affinity chromatography are agonists at the A2-adenosine receptor that mediates coronary vasodilation in the dog. The most active analogues had spacer arms terminating in -NH2, -NHCH3 or in a biotin residue. Comparisons of coronary vasoactivity with affinity for brain A1 adenosine receptors identified one biotin-containing analogue as relatively selective for coronary A2 receptors. The complex of this analogue with avidin retained coronary vasoactivity.
在N6位被设计用于连接可溶性大分子或用于亲和色谱的固体支持物的间隔臂取代的腺苷类似物，是犬体内介导冠状动脉血管舒张的A2-腺苷受体的激动剂。活性最高的类似物具有以-NH2、-NHCH3或生物素残基结尾的间隔臂。通过比较冠状动脉血管活性与对脑A1腺苷受体的亲和力，确定了一种含生物素的类似物对冠状动脉A2受体具有相对选择性。该类似物与抗生物素蛋白的复合物保留了冠状动脉血管活性。
