Hamilton H W, Taylor M D, Steffen R P, Haleen S J, Bruns R F
Department of Chemistry, Warner-Lambert/Parke-Davis Pharmaceutical Research, Ann Arbor, MI 48105.
Life Sci. 1987 Nov 16;41(20):2295-302. doi: 10.1016/0024-3205(87)90542-x.
Binding affinities of 28 adenosine analogs at A1 adenosine receptors (rat whole brain membranes, [3H]N6-cyclohexyladenosine, CHA), and at A2 adenosine receptors (rat striatal membranes, [3H]NECA) were compared to their EC25 values for decreasing heart rate and increasing coronary flow in the isolated rat heart. Heart rate (an A1 response) correlated with A1 binding affinity (r2 = 0.71, p less than 0.0001) but not with A2 binding affinity (r2 = 0.007, n.s.); conversely, coronary flow (an A2 response) correlated with A2 binding affinity (r2 = 0.83, p less than 0.0001) but not with A1 binding affinity (r2 = 0.05, n.s.). These results confirm that the brain A1 and A2 receptors, studied by binding methods, bear close similarities to their respective counterparts in the heart, studied by means of functional responses.
比较了28种腺苷类似物在A1腺苷受体（大鼠全脑膜，[3H]N6-环己基腺苷，CHA）和A2腺苷受体（大鼠纹状体膜，[3H]NECA）上的结合亲和力与其在离体大鼠心脏中降低心率和增加冠脉流量的EC25值。心率（一种A1反应）与A1结合亲和力相关（r2 = 0.71，p小于0.0001），但与A2结合亲和力无关（r2 = 0.007，无显著性差异）；相反，冠脉流量（一种A2反应）与A2结合亲和力相关（r2 = 0.83，p小于0.0001），但与A1结合亲和力无关（r2 = 0.05，无显著性差异）。这些结果证实，通过结合方法研究的脑A1和A2受体与其通过功能反应研究的心脏中各自对应的受体非常相似。
