Baker M D, Ritchie J M
Department of Pharmacology, Yale University School of Medicine, New Haven, Connecticut 06520.
Proc Biol Sci. 1994 Mar 22;255(1344):259-65. doi: 10.1098/rspb.1994.0037.
Capsaicin, a lipophilic alkaloid, blocked type I K+ currents in rabbit cultured Schwann cells when applied by superfusion. The concentration-response relation at equilibrium was well described by a rectangular hyperbola, with a KD of 8.7 microM. The kinetics of block resembled an 'inactivation', the rate of blockade increasing with increasing concentrations of capsaicin (1-100 microM). Unlike internal tetraethylammonium (TEA) ions (5-10 mM), which preferentially reduced outward current in symmetrical high [K+], capsaicin reduced both inward and outward type I current by the same proportion. The block achieved by capsaicin during a voltage-clamp step that activated the current was relieved by subsequent hyperpolarization, and the rate of relief from block at -70 mV and -100 mV could be reasonably accounted for on the assumption that capsaicin had to unbind to allow the channels' to close.
辣椒素是一种亲脂性生物碱,通过灌流法施加时可阻断兔培养雪旺细胞中的I型钾电流。平衡时的浓度-反应关系可用矩形双曲线很好地描述,解离常数(KD)为8.7微摩尔。阻断动力学类似于“失活”,阻断速率随辣椒素浓度(1-100微摩尔)的增加而增加。与内部四乙铵(TEA)离子(5-10毫摩尔)不同,后者在对称高[K+]时优先降低外向电流,辣椒素以相同比例降低内向和外向I型电流。在激活电流的电压钳制步骤中,辣椒素所实现的阻断可通过随后的超极化解除,并且在-70毫伏和-100毫伏时阻断解除的速率可以合理地解释为假设辣椒素必须解离才能使通道关闭。