Terrar D A
Br J Pharmacol. 1974 Jun;51(2):259-68. doi: 10.1111/j.1476-5381.1974.tb09656.x.
1 Microelectrodes have been used to follow changes in membrane potential at end-plate regions of frog skeletal muscle fibres exposed to carbachol; the depolarizing drug was applied to narrow strips of muscle in a rapidly flowing solution containing relatively impermeant anions rather than chloride.2 During prolonged applications of carbachol (10 to 20 muM), the depolarization caused by the drug showed a gradual decline which was attributed to desensitization.3 Desensitization was little if at all affected by supplementing the external solution with factors present in tissue-culture media, or by treating the muscle with strophanthidin (25 muM).4 The rate of repolarization in the presence of carbachol (10 to 20 muM) was greatly increased by the SKF-525A congeners pipenzolate bromide (10 muM) and adiphenine hydrochloride (1 muM). The desensitization-enhancing action of these compounds is discussed.
微电极已被用于追踪暴露于卡巴胆碱的青蛙骨骼肌纤维终板区域膜电位的变化;将去极化药物应用于快速流动溶液中的窄条肌肉,该溶液含有相对不易透过的阴离子而非氯离子。
在长时间应用卡巴胆碱(10至20μM)期间,药物引起的去极化呈现逐渐下降,这归因于脱敏作用。
通过在外部溶液中补充组织培养基中存在的因子,或用毒毛花苷(25μM)处理肌肉,脱敏作用几乎没有受到影响。
在存在卡巴胆碱(10至20μM)的情况下,SKF-525A同系物溴哌苯酯(10μM)和盐酸阿地芬宁(1μM)极大地提高了复极化速率。讨论了这些化合物增强脱敏作用的机制。