We investigated the pharmacology and voltage-dependent activation and inactivation kinetics of the 'delayed rectifier' K+ current, IdK, in canine colonic myocytes and developed protocols which separate this current into three distinct components that differ in their kinetics and pharmacology. 2. Block of IdK by TEA or 4-aminopyridine (4-AP) alone was incomplete. Maximal concentrations of TEA or 4-AP blocked 76% (EC50 = 2.6 mM) and 51% (EC50 = 69 mM) of current, respectively. In the presence of 10 mM 4-AP, IdK could be blocked completely by TEA. 3. TEA and 4-AP had distinct effects on current activation: time constants for activation of IdK at +10 mV were 25.6 +/- 4.4 ms under control conditions, 40.3 +/- 7.6 ms in the presence of 10 mM 4-AP and 16.7 +/- 2.3 ms with 10 mM TEA in the bath solution. 4-AP block and removal of block were use dependent, but no frequency dependence or voltage dependence of steady-state block could be detected. These data are consistent with the presence of a rapidly activating 4-AP-sensitive current, IdK(f), and a more slowly activating TEA-sensitive current component, IdK(s). 4. A third component of the delayed rectifier current, IdK(n), was revealed when 10 mM TEA was included in the pipette solution. IdK(n) was rapidly activating, had a membrane potential at half-maximal inactivation (V1/2) for steady-state inactivation 13 mV negative of that for the mixed IdK, was completely insensitive to 4-AP (10 mM) and was blocked by external TEA with an EC50 of 7.7 mM. 5. These data demonstrate that the delayed rectifier current in canine colonic smooth muscle is composed of three currents, IdK(f), IdK(s) and IdK(n). All three currents are insensitive to charybdotoxin (100 nM).
摘要
我们研究了犬结肠肌细胞中“延迟整流”钾电流(IdK)的药理学特性以及电压依赖性激活和失活动力学,并制定了将该电流分离为三个不同成分的方案,这些成分在动力学和药理学方面存在差异。2. 单独使用四乙铵(TEA)或4-氨基吡啶(4-AP)对IdK的阻断并不完全。TEA或4-AP的最大浓度分别阻断了76%(半数有效浓度[EC50]=2.6 mM)和51%(EC50=69 mM)的电流。在存在10 mM 4-AP的情况下,TEA可完全阻断IdK。3. TEA和4-AP对电流激活有不同影响:在+10 mV时,IdK激活的时间常数在对照条件下为25.6±4.4毫秒,在存在10 mM 4-AP时为40.3±7.6毫秒,在浴液中存在10 mM TEA时为16.7±2.3毫秒。4-AP的阻断和阻断的解除具有使用依赖性,但未检测到稳态阻断的频率依赖性或电压依赖性。这些数据与存在快速激活的4-AP敏感电流IdK(f)和激活较慢的TEA敏感电流成分IdK(s)一致。4. 当移液管溶液中包含10 mM TEA时,揭示了延迟整流电流的第三个成分IdK(n)。IdK(n)快速激活,其稳态失活的半数最大失活膜电位(V1/2)比混合的IdK负13 mV,对10 mM 4-AP完全不敏感,并且被细胞外TEA以7.7 mM的EC50阻断。5. 这些数据表明犬结肠平滑肌中的延迟整流电流由三种电流组成,即IdK(f)、IdK(s)和IdK(n)。所有这三种电流对100 nM的蝎毒素均不敏感。