Horita A, Carino M A, Chinn C
Department of Pharmacology, University of Washington School of Medicine, Seattle 98195.
Pharmacol Biochem Behav. 1988 May;30(1):115-8. doi: 10.1016/0091-3057(88)90432-7.
The intravenous administration of codeine to diazepam-narcotized rabbits resulted in a shortened duration of loss of righting reflex. Coadministration of naltrexone plus codeine enhanced this analeptic effect and was also effective in shortening the duration of pentobarbital narcosis. The analeptic effect was blocked by atropine, but not by methylatropine, indicating involvement of a central cholinergic mechanism. In rats the analeptic activity correlated with the reversal of the diazepam-induced fall in sodium dependent high affinity choline uptake in hippocampal and cortical synaptosomes. These findings may represent the pharmacological basis of the recently reported antinarcoleptic action of codeine in man.
给地西泮麻醉的兔子静脉注射可待因，导致翻正反射消失的持续时间缩短。纳曲酮与可待因联合使用增强了这种苏醒作用，并且在缩短戊巴比妥麻醉持续时间方面也有效。这种苏醒作用被阿托品阻断，但未被甲基阿托品阻断，表明涉及中枢胆碱能机制。在大鼠中，苏醒活性与地西泮诱导的海马和皮质突触体中钠依赖性高亲和力胆碱摄取下降的逆转相关。这些发现可能代表了最近报道的可待因对人抗发作性睡病作用的药理学基础。
