Yamawaki S, Carino M A, Horita A
Neurosci Lett. 1985 Mar 22;55(1):61-4. doi: 10.1016/0304-3940(85)90312-x.
Eight opiate agonists, administered by the intracerebroventricular (i.c.v.) route, were evaluated as analeptics in pentobarbital-anesthetized rabbits. Morphine, codeine, ethylketocyclazocine, N-allylnormetazocine, meperidine and methadone, but not etorphine or D-Ala2-Met-enkephalin, given i.c.v. 40 min after pentobarbital (30 mg/kg i.v.), produced significant shortening of the duration of anesthesia as determined by the loss of the righting reflex. No apparent relationship was found between this and analgesic potency, nor with the specific receptor subtypes with which these agonists are known to interact. With active compounds, such as morphine, codeine and methadone, producing narcotic sedation, it was necessary to pretreat the animals with naltrexone to unmask the analeptic effect. It is concluded that the analeptic effect produced by certain opiate drugs is not specifically related to any of the subtypes of opiate receptors thus far described.
通过脑室内（i.c.v.）途径给药的八种阿片类激动剂，在戊巴比妥麻醉的兔子中被评估为苏醒药。在静脉注射戊巴比妥（30mg/kg）40分钟后经脑室内给予吗啡、可待因、乙基酮环唑辛、N-烯丙基去甲左啡诺、哌替啶和美沙酮，但未给予埃托啡或D-Ala2-Met-脑啡肽，通过翻正反射消失测定，可显著缩短麻醉持续时间。未发现这与镇痛效力之间存在明显关系，也未发现与已知这些激动剂相互作用的特定受体亚型之间存在明显关系。对于产生麻醉性镇静作用的活性化合物，如吗啡、可待因和美沙酮，有必要用纳曲酮预处理动物以揭示其苏醒作用。得出的结论是，某些阿片类药物产生的苏醒作用与迄今为止所描述的任何阿片受体亚型均无特异性关系。
