Lingle C
J Physiol. 1983 Jun;339:419-37. doi: 10.1113/jphysiol.1983.sp014724.
The voltage dependence, concentration dependence, and agonist dependence of blocking and unblocking produced by anticholinergic agents on the ionophoretically activated cholinergic currents of the lobster gastric mill 1 (g.m.1) muscle were examined. Although the ionophoretic technique provides only qualitative information as to blocking mechanisms it is useful in revealing slow components of the blocking action of some drugs. At least two qualitatively different types of voltage-dependent block of the crustacean cholinergic currents were observed. For pempidine, mecamylamine and decamethonium (also chlorisondamine: Lingle, 1983), a slowly developing voltage-dependent block was produced that led to the formation of a stable-blocked state. Recovery from this stable-blocked state is largely dependent on subsequent application of agonist. In contrast, recovery from the voltage-dependent block produced by QX-222, atropine, procaine and curare either proceeds independently of agonist application or occurs too rapidly to be observed by the present methods. Blockade by hexamethonium reveals anomalous voltage dependence, being enhanced over some voltages and relieved with additional hyperpolarization. Blockade by trimetaphan is largely independent of membrane potential except at higher concentrations.
研究了抗胆碱能药物对龙虾胃磨肌1（g.m.1）肌肉经离子电泳激活的胆碱能电流产生的阻断和解除阻断的电压依赖性、浓度依赖性和激动剂依赖性。尽管离子电泳技术仅提供有关阻断机制的定性信息，但它有助于揭示某些药物阻断作用的缓慢成分。观察到至少两种性质不同的甲壳类动物胆碱能电流的电压依赖性阻断类型。对于潘必定、美加明和十烃季铵（氯异吲哚铵也是如此：林格尔，1983年），产生了一种缓慢发展的电压依赖性阻断，导致形成稳定的阻断状态。从这种稳定的阻断状态恢复很大程度上取决于随后激动剂的应用。相比之下，QX - 222、阿托品、普鲁卡因和箭毒产生的电压依赖性阻断的恢复要么独立于激动剂的应用进行，要么发生得太快以至于用目前的方法无法观察到。六甲铵的阻断显示出异常的电压依赖性，在某些电压下增强，额外的超极化可解除阻断。曲美芬的阻断在很大程度上与膜电位无关，除非在较高浓度下。
