Summary
To study \-adrenoceptor antagonist-induced changes in human vascular \-adrenoceptors, we determined the effects of chronic treatment with different \-adrenoceptor antagonists without intrinsic sympathomimetic activity (ISA) on \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 nonselective ß-adrenoceptor antagonists propranolol or sotalol, the density of saphenous vein \2-adrenoceptors was significantly higher than in control (i.e. patients not treated with ß-adrenoceptor antagonists), whereas in patients chronically treated with the selective \1-adrenoceptor antagonists metoprolol or bisoprolol it was not different from control. It is concluded that \-adrenoceptor antagonists without ISA increase human saphenous vein \2-adrenoceptors in a subtype-selective fashion.
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Brodde, OE., Zerkowski, HR., Doetsch, N. et al. Subtype-selective up-regulation of human saphenous vein \2-adrenoceptors by chronic \-adrenoceptor antagonist treatment. Naunyn-Schmiedeberg's Arch. Pharmacol. 339, 479–482 (1989). https://doi.org/10.1007/BF00736065
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DOI: https://doi.org/10.1007/BF00736065