Permeability of the Blood-Brain Barrier for Dilept and Its Active Metabolite

被引：0

作者：

Zherdev, V. P. ^{[1
]}

Boyko, S. S. ^{[1
]}

Mesonzhnik, N. V. ^{[1
]}

Bastrygin, D. V. ^{[1
]}

机构：

[1] Russian Acad Med Sci, VV Zakusov Inst Pharmacol, Moscow, Russia

来源：

BULLETIN OF EXPERIMENTAL BIOLOGY AND MEDICINE | 2011年 / 151卷 / 03期

关键词：

blood-brain barrier; dilept; dilept metabolite; peptide carriers; NEUROTENSIN; CLONING;

D O I：

10.1007/s10517-011-1322-z

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

Experiments on rats with measurements by HPLC-MS/MS showed that antipsychotic preparation dilept (N-caproyl-L-prolyl-L-tyrosine methyl ester) administered per os in doses of 40 and 200 mg/kg crossed the blood-brain barrier and was detected in rat brain (unchanged drug and its active metabolite N-caproyl-L-prolyl-L-tyrosine). The brain/plasma distribution coefficient for dilept was 2.0, for metabolite 0.5. No dose-concentration relationship was found, presumably because of the high dose of the drug transported from the blood to the brain not only by free diffusion, but also with participation of active carriers, whose number was limited.

引用

页码：330 / 332

页数：3

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