Ayre S G, Skaletski B, Mosnaim A D
Department of Family Medicine, University of Health Sciences, Chicago Medical School, IL 60064.
Res Commun Chem Pathol Pharmacol. 1989 Jan;63(1):45-52.
Azidothymidine (AZT) crosses the blood-brain barrier (BBB) of 6-8 week old Sprague-Dawley male white rats (Oldendorf technique, ipsilateral cerebral hemisphere) with a brain-uptake index (BUI) of 5.4 +/- 0.8 (mean +/- S.D., n = 13, range 4.4-6-6) using 14C-antipyrine as the diffusible standard. Pretreatment of the animals with the higher doses of insulin (0.6 or 1.0, but not 0.1, 0.2, or 0.3 units per rat, 3 or 10 min. before decapitation) resulted in higher values for the BUI of AZT in most individual animals. In the group of rats treated with 1.0 unit of insulin 10 min. before decapitation, a statistically significant increase in the BUI was observed. Some possible clinical applications of this pharmacologic strategy are discussed.
叠氮胸苷（AZT）可穿过6 - 8周龄的斯普拉格 - 道利雄性白鼠的血脑屏障（采用奥尔德恩多夫技术，同侧脑半球），以14C - 安替比林作为可扩散标准时，脑摄取指数（BUI）为5.4±0.8（平均值±标准差，n = 13，范围4.4 - 6.6）。用较高剂量胰岛素（每只大鼠0.6或1.0单位，但不是0.1、0.2或0.3单位，在断头前3或10分钟）对动物进行预处理，导致大多数个体动物的AZT的BUI值更高。在断头前10分钟用1.0单位胰岛素处理的大鼠组中，观察到BUI有统计学上的显著增加。讨论了这种药理学策略的一些可能的临床应用。
