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首页> 外文期刊>Acta Pharmacologica Sinica >Tetrahydroacridine inhibits voltage-dependent Na~+ current in guinea-pig ventricular myocytes
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Tetrahydroacridine inhibits voltage-dependent Na~+ current in guinea-pig ventricular myocytes

机译：四氢ac啶抑制豚鼠心室肌​​细胞中电压依赖性Na〜+电流

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AIM: To study the effects of tetrahydroacridine (tacrine) on voltage-gated Na~+ channels in cardiac tissues. METHODS: Single ventricular myocytes were enzymatically dissociated from adult guinea-pig heart. Voltage-dependent Na~+ current was recorded using whole cell voltage-clamp technique. RESULTS: (1) Tacrine reversibly inhibited Na~+ current with an IC_(50) value of 120 μmol/L (95 % confidence range: 108-133 μmol/L). (2) The inhibitory effects of tacrine on Na~+ current exhibited both a tonic nature and use-dependence. (3) Tacrine at 100 μmol/L caused a negative shift (about 10 mV) in the voltage-dependence of steady-state inactivation of Na~+ current, and retarded its recovery from inactivation, but did not affect its activation curve. (4) Intracellular application of tacrine significantly inhibited Na~+ current. CONCLUSION: In addition to blocking other voltage-gated ion channels, tacrine blocked Na~+ channels in guinea-pig ventricular myocytes. Tacrine acted as inactivation stabilizer of Na~+ channels in cardiac tissues.
机译：目的：研究四氢ac啶（他克林）对心脏组织电压门控Na〜+通道的影响。方法：将成年豚鼠心脏中的单个心室肌细胞酶解。使用全电池电压钳技术记录电压依赖性Na〜+电流。结果：（1）他克林可逆地抑制Na〜+电流，IC_（50）值为120μmol/ L（95％置信范围：108-133μmol/ L）。 （2）他克林对Na〜+电流的抑制作用表现为强直性和使用依赖性。 （3）他克林在100μmol/ L时引起Na〜+稳态失活的电压依赖性为负移（约10 mV），并阻碍了其从失活的恢复，但不影响其活化曲线。 （4）细胞内使用他克林可显着抑制Na〜+电流。结论：他克林除了阻断其他电压门控离子通道外，还阻断了豚鼠心室肌​​细胞中的Na〜+通道。他克林是心脏组织中Na〜+通道的失活稳定剂。

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