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Structure—activity relationships forin vitrooxime reactivation of chlorpyrifos-inhibited acetylcholinesterase

✍ Scribed by K. Kuča; V. Račáková; D. Jun

Book ID: 111491055
Publisher: Versita
Year: 2007
Tongue: English
Weight: 187 KB
Volume: 61
Category: Article
ISSN: 0366-6352
DOI: 10.2478/s11696-007-0030-7

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✦ Synopsis

Abstract

Organophosphorus pesticides parathion, chlorpyrifos, and malathion inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7) via phosphorylation of its active site. AChE reactivators and anticholinergics are compounds used as antidotes in the case of intoxication by these AChE inhibitors. In this work, chlorpyrifos, a representative member of this pesticide family, was used to inhibit the AChE activity of rat brain. The effect of twenty-one structurally different AChE reactivators was tested in vitro and subsequently, the relationship between their chemical structure and biological activity was outlined.

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