Blocking Effect of Bepridil on Na^+/Ca^<2+> Exchange Current in Guinea Pig Cardiac Ventricular Myocytes
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概要
- 論文の詳細を見る
We examined the effect of bepridil, a class IV antiarrhythmic drug, on Na+/Ca2+ exchange current (INCX) in single guinea pig cardiac ventricular cells using the whole-cell voltage clamp technique. INCX was recorded by ramp pulses from the holding potential of −60 mV in the presence of 140 mM Na+ and 1 mM Ca2+ in the external solution and 20 mM Na+ and 119 nM free Ca2+ (7 mM Ca2+ and 20 mM BAPTA) in the internal solution. Bepridil suppressed INCX in a concentration-dependent manner. The IC50 value was 8.1 μM with a Hill coefficient of 0.8. Intracellular treatment with trypsin via the pipette solution attenuated the blocking effect of bepridil, suggesting that the inhibitory site is on the cytosolic side of the Na+/Ca2+ exchanger. In the absence of albumin in the external solution, 10 μM bepridil inhibited INCX by 46 ± 7% (n = 8), while bepridil blocked it by 28 ± 8% (n = 6) in the presence of albumin. Bepridil inhibited INCX in a supra-therapeutic concentration range.
- 社団法人 日本薬理学会の論文
- 2001-04-01
著者
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Kimura Junko
Department of Analytical Chemistry, Faculty of Pharmaceutical Sciences, Toho University
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Watanabe Yasuhide
Department of Basic Nursing, Hamamatsu University School of Medicine
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Watanabe Yasuhide
Div. Of Pharmacological Sci. Dep. Of Health Sci. Hamamatsu Univ. School Of Medicine Jpn
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Watanabe Yasuhide
Department Of Applied Biological Chemistry Faculty Of Agriculture Shizuoka University
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Kimura Junko
Dep. Of Pharmacology School Of Medicine Fukushima Medical Univ. Jpn
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Kimura J
Department Of Pharmacology Fukushima Medical University School Of Medicine
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Kimura Junko
Department Of Ecology And Clinical Therapeutics School Of Nursing And Department Of Pharmacology Sch
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