Molenaar P, Jones C R, McMartin L R, Summers R J
Department of Pharmacology, University of Melbourne, Parkville, Victoria, Australia.
J Pharmacol Exp Ther. 1988 Jul;246(1):384-93.
The location and proportions of beta-1 and beta-2 adrenoceptors in canine coronary arteries (0.5-2 mm) has been examined by autoradiography. X-ray film and nuclear emulsion-coated coverslips were exposed to sections of coronary artery previously incubated with [125I]iodocyanopindolol (50 pM) in the absence and presence of ICI 118,551 (70 nM) to block beta-2 adrenoceptors, CGP 20712A (100 nM) to block beta-1 adrenoceptors or (-)-propranolol (1 microM) to define nonspecific binding. The medial smooth muscle of the coronary artery had an even distribution of beta-1 adrenoceptors and two populations of beta-2 adrenoceptors, one evenly distributed and the other highly localized. Beta-2 adrenoceptors were also located on nerve tissue and in the adventitia. There was no evidence for localization of beta adrenoceptors on endothelial cells. Quantitative autoradiography was performed using computer-assisted image processing and the program AVID. The binding of [125I]cyanopindolol was saturable (KD = 50 pM) and competition binding curves with the beta-1 selective antagonist CGP 20712A and beta-2 selective antagonist ICI 118,551 showed beta-1 and beta-2 adrenoceptors in the proportions of 85:15% in both 0.5- and 2-mm arteries.
采用放射自显影法研究了犬冠状动脉(0.5 - 2毫米)中β-1和β-2肾上腺素能受体的位置及比例。将X射线胶片和涂有核乳胶的盖玻片暴露于预先在不存在和存在ICI 118,551(70 nM)以阻断β-2肾上腺素能受体、CGP 20712A(100 nM)以阻断β-1肾上腺素能受体或(-)-普萘洛尔(1 μM)以确定非特异性结合的情况下,与[125I]碘氰吲哚洛尔(50 pM)孵育过的冠状动脉切片。冠状动脉的中层平滑肌有均匀分布的β-1肾上腺素能受体和两类β-2肾上腺素能受体,一类均匀分布,另一类高度集中。β-2肾上腺素能受体也位于神经组织和外膜中。没有证据表明β肾上腺素能受体定位于内皮细胞上。使用计算机辅助图像处理和AVID程序进行定量放射自显影。[125I]氰吲哚洛尔的结合是可饱和的(KD = 50 pM),与β-1选择性拮抗剂CGP 20712A和β-2选择性拮抗剂ICI 118,551的竞争结合曲线显示,在0.5毫米和2毫米的动脉中,β-1和β-2肾上腺素能受体的比例均为85:15%。