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通过生物膜实现的递送改善。3. 以二氢吡啶前药形式通过血脑屏障递送N-甲基吡啶-2-甲醛肟氯化物。

Improved delivery through biological membranes. 3. Delivery of N-methylpyridinium-2-carbaldoxime chloride through the blood-brain barrier in its dihydropyridine pro-drug form.

作者信息

Shek E, Higuchi T, Bodor N

出版信息

J Med Chem. 1976 Jan;19(1):113-7. doi: 10.1021/jm00223a019.

DOI:10.1021/jm00223a019
PMID:1246032
Abstract

Administration of N-methyl-1,6-dihydropyridine-2-carbaldoxime hydrochloride, the pro-drug form of 2-PAM, resulted in an average of 13-fold increase in the amount of 2-PAM delivered into the brain of mice as compared to the administration of 2-PAM. The pro-drug which crossed the BBB resulted in a dramatic increase in the reactivation of AChE blocked by DFP. In vivo studies of the "aging" of the phosphorylated AChE in the brain of mice could also be studied using pro-2-PAM.

摘要

给予N-甲基-1,6-二氢吡啶-2-甲醛肟盐酸盐(2-PAM的前药形式),与给予2-PAM相比,进入小鼠脑内的2-PAM量平均增加了13倍。穿过血脑屏障的前药导致被二异丙基氟磷酸酯(DFP)阻断的乙酰胆碱酯酶(AChE)再活化显著增加。使用前体2-PAM也可以研究小鼠脑中磷酸化AChE“老化”的体内研究。

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Proceedings of the British Pharmacological Society. 17th-19th December, 1979: University of London (Institute of Education).英国药理学会会议记录。1979年12月17日至19日:伦敦大学(教育学院)
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