Lister R G, Nutt D J
Division of Intramural Clinical and Biological Research, National Institute on Alcohol Abuse and Alcoholism, Bethesda, MD 20892.
Adv Alcohol Subst Abuse. 1988;7(3-4):119-23. doi: 10.1300/J251v07n03_19.
It has recently been claimed that RO 15-4513 selectively opposes some of the behavioral actions of ethanol. Our studies on the intrinsic effects of this compound have shown it to be proconvulsant and to reduce exploratory behavior in mice. In these respects RO 15-4513 resembles a benzodiazepine receptor partial inverse agonist. Such intrinsic actions may well explain its alcohol-antagonizing properties, and argue against its potential in humans. In addition to partially reversing the effects of ethanol, RO 15-4513 also partially reverses the behavioral effect of a barbiturate and completely reverses the effects of a benzodiazepine.
最近有人声称RO 15 - 4513能选择性地对抗乙醇的某些行为作用。我们对该化合物内在作用的研究表明，它会诱发惊厥并减少小鼠的探索行为。在这些方面，RO 15 - 4513类似于苯二氮䓬受体部分反向激动剂。这种内在作用很可能解释了它的酒精拮抗特性，也表明其在人体应用方面存在问题。除了能部分逆转乙醇的作用外，RO 15 - 4513还能部分逆转巴比妥酸盐的行为效应，并完全逆转苯二氮䓬类药物的效应。
