PMID: 11907159Mar 22, 2002Paper

Differential effects of bucindolol and carvedilol on noradenaline-induced hypertrophic response in ventricular cardiomyocytes of adult rats

The Journal of Pharmacology and Experimental Therapeutics
Klaus PönickeOtto-Erich Brodde

Abstract

In adult rat ventricular cardiomyocytes, noradrenaline exerts dual effects on protein synthesis: increases via alpha(1)-adrenoceptors and decreases via beta(1)-adrenoceptors. Carvedilol and bucindolol are beta-blockers with additional alpha(1)-adrenoceptor blocking activities. We studied the effects of carvedilol and bucindolol on noradrenaline-induced protein synthesis (assessed by [(3)H]phenylalanine incorporation) in adult rat ventricular cardiomyocytes. Radioligand binding studies with [(125)I]iodocyanopindolol and [(3)H]prazosin revealed that carvedilol had a much higher affinity to alpha(1)-adrenoceptors than bucindolol (beta(1)-/alpha(1)-adrenoceptor ratio for carvedilol, 1:2.7; for bucindolol, 1:43). Noradrenaline-evoked increases in protein synthesis were enhanced by propranolol (1 microM) and beta(1)-adrenoceptor-selective antagonists bisoprolol (1 microM) and CGP 20712A [1-[2-((3-carbamoyl-4-hydroxy)phenoxy)-ethyl-amino]-3-[4-(1-methyl-4-trifluoromethyl-2-imidazolyl)phenoxy]-2-propranol methanesulfonate] (300 nM). Carvedilol (100 pM-10 microM) inhibited 1 microM noradrenaline-induced increase in protein synthesis with monophasic concentration-inhibition curves independent of whether CGP 20712A was present or not; K(i...Continue Reading

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Jan 1, 1992·Journal of Cardiovascular Pharmacology·M R BristowB Müller-Beckmann
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Jun 2, 2001·The New England Journal of Medicine·E Braunwald

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Citations

May 1, 2012·Biophysical Chemistry·Cédric Fiez-VandalMyriam Duckely
Jul 27, 2010·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Grazyna GroszekBarbara Filipek
May 1, 2008·The Journal of Pharmacology and Experimental Therapeutics·Aida SalamehDietrich Pfeiffer
Jul 31, 2019·Oxidative Medicine and Cellular Longevity·Bruna Gazzi de Lima-SeolinNeelam Khaper
Dec 15, 2005·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·A SalamehS Dhein

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