Marangos P J
J Recept Res. 1984;4(1-6):231-44. doi: 10.3109/10799898409042552.
The characteristics of adenosine receptors and adenosine uptake sites in brain are presented. High affinity adenosine receptors of the A1 type bind [3H]cyclohexyladenosine ([3H]CHA) and [3H]diethyl-phenyl-xanthine ([3H]DPX) with 10(-9) potency while adenosine uptake sites are labeled 10(-10) potency with [3H]nitrobenzylthioinosine ([3H]NBI). NBI does not inhibit either [3H]CHA (agonist) or [3H]DPX (antagonist) binding to adenosine receptors in brain cortical membranes and conversely CHA and other adenosine receptor ligands are very poor inhibitors of [3H]NBI binding to adenosine uptake sites. A number of other differences between the receptor and uptake site are discussed which provide rather strong evidence that these two sites are quite distinct and that the labeled ligands used represent specific probes for each site.
本文介绍了大脑中腺苷受体和腺苷摄取位点的特征。A1型高亲和力腺苷受体与[3H]环己基腺苷（[3H]CHA）和[3H]二乙苯基黄嘌呤（[3H]DPX）结合的亲和力为10^(-9)，而腺苷摄取位点用[3H]硝基苄硫肌苷（[3H]NBI）标记的亲和力为10^(-10)。NBI不抑制[3H]CHA（激动剂）或[3H]DPX（拮抗剂）与大脑皮质膜中腺苷受体的结合，相反，CHA和其他腺苷受体配体对[3H]NBI与腺苷摄取位点的结合抑制作用很差。文中还讨论了受体和摄取位点之间的许多其他差异，这些差异提供了相当有力的证据，表明这两个位点截然不同，且所使用的标记配体分别代表每个位点的特异性探针。
