BRL 38227对大鼠门静脉钾电流的调控特性
Characterization of potassium currents modulated by BRL 38227 in rat portal vein.
作者信息
Noack T, Deitmer P, Edwards G, Weston A H
机构信息
Department of Physiology, Philipps University, Marburg, Germany.
出版信息
Br J Pharmacol. 1992 Jul;106(3):717-26. doi: 10.1111/j.1476-5381.1992.tb14400.x.
Abstract
- Smooth muscle cells of the rat portal vein were dispersed by enzymatic treatment and recordings of whole-cell membrane potassium currents were made by the voltage-clamp technique. In isolated cells by use of combined voltage- and current-clamp the effect of BRL 38227 on membrane potential and ionic currents was also studied. 2. BRL 38227 (0.1 to 10 microM) induced a non-inactivating potassium current (IKCO) which developed slowly (900 s to 300 s, respectively) to its full size. These effects of BRL 38227 were reversible. 3. In addition to its K-channel opening properties, BRL 38227 (1 to 10 microM) inhibited the amplitude and changed the activation and inactivation characteristics of a slowly-inactivating, calcium influx-independent, outward potassium current (I(TO)). 4. Application of stationary fluctuation analysis to IKCO, showed a mean single channel current of 0.65 pA at -10 mV under a quasi-physiological potassium gradient. 5. In a combined voltage-clamp/current-clamp configuration, BRL 38227 (1 microM) induced a mean hyperpolarization of 22 mV. 6. The induction of IKCO by BRL 38227 and the associated hyperpolarization were suppressed by glibenclamide (1 to 10 microM) in a concentration-dependent manner. Glibenclamide (1 microM) had no effect on the inhibition of I(TO) by BRL 38227 (1 microM).
摘要
- 通过酶处理分散大鼠门静脉的平滑肌细胞，并采用电压钳技术记录全细胞膜钾电流。在使用电压钳和电流钳相结合的分离细胞中，还研究了BRL 38227对膜电位和离子电流的影响。2. BRL 38227（0.1至10微摩尔）诱导出一种非失活钾电流（IKCO），该电流发展缓慢（分别为900秒至300秒）至其全尺寸。BRL 38227的这些作用是可逆的。3. 除了其钾通道开放特性外，BRL 38227（1至10微摩尔）还抑制了一种缓慢失活、与钙内流无关的外向钾电流（I(TO)）的幅度，并改变了其激活和失活特性。4. 对IKCO应用静态波动分析，发现在准生理钾梯度下，-10 mV时平均单通道电流为0.65皮安。5. 在电压钳/电流钳联合配置中，BRL 38227（1微摩尔）诱导平均超极化22 mV。6. 格列本脲（1至10微摩尔）以浓度依赖的方式抑制了BRL 38227诱导的IKCO及其相关的超极化。格列本脲（1微摩尔）对BRL 38227（1微摩尔）对I(TO)的抑制作用无影响。
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