The effects of SKF 525-A on the analgesic and barbiturate-potentiating activity of delta 9-tetrahydrocannabinol in mice and rats.
The effects of SKF 525-A on the analgesic and barbiturate-potentiating activity of delta 9-tetrahydrocannabinol in mice and rats.
复制标题
SKF 525-A 对小鼠和大鼠中 δ 9-四氢大麻酚的镇痛和巴比妥酸盐增强活性的影响。
作者：
R. Sofia;H. Barry
δ 9-四氢大麻酚（THC）能显著延长小鼠和大鼠的巴比妥钠睡眠时间。当动物用SKF 525-A（一种负责药物代谢的肝微粒体酶的非特异性抑制剂）预处理时，这种作用的幅度和持续时间显著增强。此外，根据所用的方法和动物种类，发现THC的镇痛效力是吗啡SO 4的一半（小鼠热板），三分之一（小鼠甩尾）和八分之一（大鼠甩尾）。然而，SKF 525-A预处理显著增强了小鼠的镇痛活性。这些数据表明，完整的THC而不一定是代谢物是观察到的CNS镇静和镇痛作用的主要原因。
delta 9-Tetrahydrocannabinol (THC) markedly potentiated barbital Na sleeping time in mice and rats. The magnitude and duration of this effect were markedly enhanced when the animals were pretreated with SKF 525-A, a nonspecific inhibitor of liver microsomal enzymes responsible for drug metabolism. Moreover, depending on the method and species of animal used, THC was found to be one half (mouse hot plate), one third (mouse tail flick), and one eighth (rat tail flick) as potent an analgesic as morphine SO4. However, pretreatment with SKF 525-A significantly potentiated the analgesic activity in mice. These data suggest that intact THC and not necessarily a metabolite(s) is principally responsible for the CNS depressant and analgesic effects observed.