Brodde O E, Zerkowski H R, Doetsch N, Khamssi M
Biochemisches Forschungslabor, Medizinische Klinik und Poliklinik, Abteilung für Nieren- und Hochdruckkranke, Universitätsklinikum, Essen, Federal Republic of Germany.
Naunyn Schmiedebergs Arch Pharmacol. 1989 Apr;339(4):479-82. doi: 10.1007/BF00736065.
To study beta-adrenoceptor antagonist-induced changes in human vascular beta-adrenoceptors, we determined the effects of chronic treatment with different beta-adrenoceptor antagonists without intrinsic sympathomimetic activity (ISA) on beta 2-adrenoceptor density (assessed by (-)-[125I]-iodopindolol binding) in human saphenous vein membranes obtained from patients undergoing coronary artery bypass grafting. In patients chronically treated with the non-selective beta-adrenoceptor antagonists propranolol or sotalol, the density of saphenous vein beta 2-adrenoceptors was significantly higher than in control (i.e. patients not treated with beta-adrenoceptor antagonists), whereas in patients chronically treated with the selective beta 1-adrenoceptor antagonists metoprolol or bisoprolol it was not different from control. It is concluded that beta-adrenoceptor antagonists without ISA increase human saphenous vein beta 2-adrenoceptors in a subtype-selective fashion.