PMID: 8974046Oct 1, 1996Paper

Beta 2-adrenoceptor activation by zinterol causes protein phosphorylation, contractile effects and relaxant effects through a cAMP pathway in human atrium

Molecular and Cellular Biochemistry
A J KaumannErnst-Georg Krause

Abstract

Evidence from ventricular preparations of cat, sheep, rat and dog suggests that both beta 1-adrenoceptors (beta 1AR) and beta 2-adrenoceptors (beta 2AR) mediate positive inotropic effects but that only beta 1AR do it through activation of a cAMP pathway. On the other hand, our evidence has shown that both beta 1AR and beta 2AR hasten relaxation of isolated human myocardium consistent with a common cAMP pathway. We have now investigated in the isolated human right atrial appendage, a tissue whose beta-AR comprise around 2/3 of beta 1AR and 1/3 of beta 2AR, whether or not beta 2AR-mediated effects occur via activation of a cAMP pathway. We carried out experiments on atria obtained from patients without advanced heart failure undergoing open heart surgery. To activate beta 2AR, we used the beta 2AR-selective ligand zinterol. Experiments were carried out on paced atrial strips (1 Hz) and tissue homogenates and membrane particles. Zinterol caused positive inotropic and lusitropic (i.e. reduction of t1/2 of relaxation) effects with EC50 values of 3 and 2 nM, respectively. The zinterol-evoked effects were unaffected by the beta 1AR-selective antagonist CGP 20712A (300 nM) but blocked surmountably by the beta 2AR-selective antagonist I...Continue Reading

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Citations

Sep 25, 1998·Cardiovascular Research·S T Rapundalo
Apr 24, 2004·Anesthesia and Analgesia·John V BoothUNKNOWN Duke Heart Center Perioperative Desensitization Group
Apr 8, 2006·Naunyn-Schmiedeberg's Archives of Pharmacology·Dana S HutchinsonTore Bengtsson
Jun 18, 2002·The Journal of Biological Chemistry·Jason D KiltsMadan M Kwatra
Aug 10, 2006·Stress : the International Journal on the Biology of Stress·Iraídes N Santos, Regina C Spadari-Bratfisch
Nov 26, 1999·Circulation Research·R P XiaoE G Lakatta
Oct 25, 2003·Journal of Cardiovascular Pharmacology·Jason D KiltsMadan M Kwatra
Aug 24, 2007·Clinical and Experimental Pharmacology & Physiology·P MolenaarA J Kaumann
Mar 10, 1999·The American Journal of Physiology·F Schröder, S Herzig
Sep 20, 2000·American Journal of Physiology. Heart and Circulatory Physiology·Z NagykaldiB Szabo
Jul 27, 1999·The Journal of Biological Chemistry·M KuschelR P Xiao
Jan 25, 2006·British Journal of Pharmacology·Peter MolenaarWilliam A Parsonage
Apr 14, 2006·Journal of Pharmacological Sciences·Otto-Erich BroddeKirsten Leineweber
Jan 13, 2011·Cardiovascular Drugs and Therapy·Ruduwaan SalieAmanda Lochner
May 1, 2021·Pharmacology Research & Perspectives·Alexander DashwoodPeter Molenaar
Jun 29, 2004·Trends in Pharmacological Sciences·Rui-Ping XiaoHeping Cheng
Jun 28, 2005·Pharmacology & Therapeutics·Ming ZhengRui-Ping Xiao
May 16, 2006·Trends in Pharmacological Sciences·Rui-Ping XiaoQide Han

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