Subtype-selective up-regulation of human saphenous vein beta 2-adrenoceptors by chronic beta-adrenoceptor antagonist treatment.
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.
Brodde
O E
OE
Biochemisches Forschungslabor, Medizinische Klinik und Poliklinik, Abteilung für Nieren- und Hochdruckkranke, Universitätsklinikum, Essen, Federal Republic of Germany.
Zerkowski
H R
HR
Doetsch
N
N
Khamssi
M
M
D000319:Adrenergic beta-Antagonists / Q000494:pharmacology*; D000328:Adult; D000368:Aged; D005260:Female; D006165:Guanylyl Imidodiphosphate / Q000494:pharmacology; D006801:Humans; D066298:In Vitro Techniques; D020120:Iodocyanopindolol; D008297:Male; D008875:Middle Aged; D009131:Muscle, Smooth, Vascular / Q000187:drug effects*; D010869:Pindolol / Q000031:analogs & derivatives; D011943:Receptors, Adrenergic, beta / Q000187:drug effects*; D012501:Saphenous Vein / Q000187:drug effects
D000319:Adrenergic beta-Antagonists; D011943:Receptors, Adrenergic, beta; D006165:Guanylyl Imidodiphosphate; D020120:Iodocyanopindolol; D010869:Pindolol