IN VITRO SCREENING OF BLOOD-BRAIN BARRIER PENETRATION OF MONOQUATERNARY ACETYLCHOLINESTERASE REACTIVATORS

被引：9

作者：

Karasova, Jana Zdarova ^{[1
]}

Stodulka, Petr ^{[2
]}

Pohanka, Miroslav ^{[2
]}

Kuca, Kamil ^{[1
,2
,3
]}

机构：

[1] Univ Def, Dept Toxicol, Fac Mil Hlth Sci, Hradec Kralove, Czech Republic

[2] Univ Def, Ctr Adv Studies, Fac Mil Hlth Sci, Hradec Kralove, Czech Republic

[3] JE Purki Nje Univ, Fac Sci, Dept Chem, Usti Nad Labem, Czech Republic

来源：

ANALYTICAL LETTERS | 2010年 / 43卷 / 09期

关键词：

Blood-brain barrier; Immobilized artificial membrane; PAM; ARTIFICIAL MEMBRANE PHOSPHATIDYLCHOLINE; MOLECULAR-SURFACE AREA; CHOLINESTERASE REACTIVATORS; DRUG ABSORPTION; OXIMES; COLUMN; ENTRY;

D O I：

10.1080/00032710903502082

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

The HPLC method for prediction of drug penetration into the CNS was examined in our study. In this in vitro study, we determined the ability of monoquaternary AChE reactivators to penetrate through blood-brain barrier (BBB). Three reactivators varying in the position of oxime group on the pyridinium ring (2-PAM, 3-PAM and 4-PAM) were evaluated. As a result, the position of the oxime group on the pyridine ring plays a role for penetration of oximes into brain. The best position of oxime group seems to be position four. The location on the position two and three is not favorable for penetrating through BBB.

引用

页码：1516 / 1524

页数：9

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