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Inhibitory Mechanism of Carvedilol on L-type Ca^(2+) Current in Rat Ventricular Myocytes

Inhibitory Mechanism of Carvedilol on L-type Ca^(2+) Current in Rat Ventricular Myocytes
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摘要 Objectives The effects of car-vedilol on calcium current (ICa) were investigated inisolated adult rat ventricular myocytes. Methods ICawas recorded by using whole-cell patch-clamp recordingtechnique. Results Carvedilol reversibly inhibited ICain a concentration-dependent manner, carvedilol at 0.1,0.3, 1 and 10 μmol/L in the extracellular solution dec-reased peak ICa by 1.52%, 18.04%, 37.34%and72.18%,respectively. The steady-state inactivation curve of ICawas shifted to more negative potentials, while the activ-ation curve was not altered. The recovery from inactiva-tion was shifted to right direction, it could not berecovered completely. In addition, Pretreatment ofventricular myocytes with prazosin and propranololcouldn't block the carvedilol-induced reduction of ICa.Conclusions Carvedilol inhibits I C a i n adult ratventricular myocytes by mechanisms involvingpreferential interaction with the inactivated state ofcalcium channel. Objectives The effects of car-vedilol on calcium current (ICa) were investigated inisolated adult rat ventricular myocytes. Methods ICawas recorded by using whole-cell patch-clamp recordingtechnique. Results Carvedilol reversibly inhibited ICain a concentration-dependent manner, carvedilol at 0.1,0.3, 1 and 10 μmol/L in the extracellular solution dec-reased peak ICa by 1.52%, 18.04%, 37.34%and72.18%,respectively. The steady-state inactivation curve of ICawas shifted to more negative potentials, while the activ-ation curve was not altered. The recovery from inactiva-tion was shifted to right direction, it could not berecovered completely. In addition, Pretreatment ofventricular myocytes with prazosin and propranololcouldn't block the carvedilol-induced reduction of ICa.Conclusions Carvedilol inhibits I C a i n adult ratventricular myocytes by mechanisms involvingpreferential interaction with the inactivated state ofcalcium channel.
出处 《South China Journal of Cardiology》 CAS 2005年第1期1-4,15,共5页 岭南心血管病杂志(英文版)
关键词 Carvedilol Whole-cell patch clamptechnique Calcium current (ICa) Carvedilol Whole-cell patch clamptechnique Calcium current (ICa)
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  • 1Dr. R. R. Ruffolo Ph.D.,M. Gellai,J. P. Hieble,R. N. Willette,A. J. Nichols.The pharmacology of carvedilol[J].European Journal of Clinical Pharmacology.1990(2)
  • 2O. P. Hamill,A. Marty,E. Neher,B. Sakmann,F. J. Sigworth.Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches[J].Pflügers Archiv European Journal of Physiology.1981(2)

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