Hunt W A, Majchrowicz E
J Pharmacol Exp Ther. 1980 Apr;213(1):9-12.
Considerable evidence both in vitro and in vivo suggests that alcohols exert their intoxicating properties through an interaction with membranes. A wide range of alcohols and diols with divergent structures induce a virtually identical spectrum of intoxication signs. Because of their pharmacological similarities to ethanol, a number of aliphatic diols were tested to determine whether this class of compounds may have efficacy in suppressing the ethanol withdrawal syndrome in rats. All of the diols tested, when administered intragastrically, were effective without inducing intoxication. Furthermore, the withdrawal-suppressing potencies of these drugs were related to their ability to partition into membranes, the same property that determines their potency as depressants. Two halogenated hydrocarbons, which are amphiphiles like alcohols and diols, were both able to suppress the withdrawal syndrome, although several aliphatic hydrocarbons could not. The data suggest that short-chain aliphatic alcohols and diols may have a common site of action, possibly in a region in membranes near the aqueous membrane interphase.
大量的体外和体内证据表明,醇类通过与膜相互作用发挥其致醉特性。一系列结构各异的醇类和二醇类会引发几乎相同的中毒症状谱。由于它们在药理学上与乙醇相似,因此对多种脂肪族二醇进行了测试,以确定这类化合物是否可能有效抑制大鼠的乙醇戒断综合征。所有经测试的二醇类,经胃内给药后均有效且不会引起中毒。此外,这些药物的戒断抑制效力与其分配到膜中的能力有关,而这一特性同样决定了它们作为抑制剂的效力。两种卤代烃,它们与醇类和二醇类一样都是两亲分子,都能够抑制戒断综合征,尽管几种脂肪族烃类不能。数据表明,短链脂肪族醇类和二醇类可能具有共同的作用位点,可能位于膜中靠近水膜界面的区域。