二异丙基氟磷酸酯对阿片类药物进入小鼠脑内的不同影响。

Different effects of di-isopropylfluorophosphate on the entry of opioids into mouse brain.

作者信息

Green P G, Kitchen I

出版信息

Br J Pharmacol. 1985 Mar;84(3):657-61. doi: 10.1111/j.1476-5381.1985.tb16147.x.

DOI:10.1111/j.1476-5381.1985.tb16147.x

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC1987147/

Abstract

Di-isopropylfluorophosphate (DFP) potentiates the antinociceptive activity of alfentanil but has no effect on the activity of morphine or fentanyl. We have studied the effect of DFP on the distribution of these three opioids in the brain. Distribution studies were carried out using 3H-labelled opioids administered subcutaneously to mice. Animals were killed at times of peak antinociceptive activity and 3H-opioid measured in plasma and in eight brain regions. DFP pretreatment (1 mg kg-1) caused a significant increase in the brain:plasma ratio of alfentanil in all brain regions but had no effect on brain:plasma ratios for morphine or fentanyl. The enhanced entry of alfentanil into the brain of DFP-treated mice probably accounts for the increased antinociception observed with this opioid. This drug interaction appears to be opioid specific.

摘要

二异丙基氟磷酸酯（DFP）可增强阿芬太尼的镇痛活性，但对吗啡或芬太尼的活性无影响。我们研究了DFP对这三种阿片类药物在脑部分布的影响。分布研究是通过给小鼠皮下注射3H标记的阿片类药物来进行的。在镇痛活性达到峰值时处死动物，并测定血浆和八个脑区中的3H-阿片类药物。DFP预处理（1 mg kg-1）导致所有脑区中阿芬太尼的脑：血浆比值显著增加，但对吗啡或芬太尼的脑：血浆比值无影响。DFP处理的小鼠脑中阿芬太尼进入量的增加可能解释了使用这种阿片类药物时观察到的镇痛作用增强。这种药物相互作用似乎具有阿片类药物特异性。

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本文引用的文献

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Tissue redistribution of fentanyl and termination of its effects in rats.芬太尼在大鼠体内的组织再分布及其作用的终止

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