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有机氯和拟除虫菊酯类杀虫剂的毒性作用机制及构效关系

Mechanisms of toxic action and structure-activity relationships for organochlorine and synthetic pyrethroid insecticides.

作者信息

Coats J R

机构信息

Department of Entomology, Iowa State University, Ames 50011-3140.

出版信息

Environ Health Perspect. 1990 Jul;87:255-62. doi: 10.1289/ehp.9087255.

Abstract

The mechanisms and sites of action of organochlorine (DDT-types and chlorinated alicyclics) and synthetic pyrethroid insecticides are presented with discussion of symptoms, physiological effects, and selectivity. The structural requirements for toxicity are assessed, and structure-activity relationships are considered for each subclass. Lipophilicity is important for all the groups because it facilitates delivery of these neurotoxicants to the site of action in the nerve. Steric factors including molecular volume, shape, and isomeric configuration greatly influence toxicity. Electronic parameters also have been demonstrated to affect biological activity in some of the groups of insecticides, e.g., Hammett's sigma and Taft's sigma * as indicators of electronegativity. New synthetic pyrethroids continue to be developed, with varied structures and different physicochemical and biological properties.

摘要

本文介绍了有机氯(滴滴涕类和氯代脂环族化合物)和拟除虫菊酯类合成杀虫剂的作用机制和作用部位,并讨论了其症状、生理效应和选择性。评估了毒性的结构要求,并考虑了每个子类的构效关系。亲脂性对所有这些杀虫剂类别都很重要,因为它有助于这些神经毒物传递到神经中的作用部位。包括分子体积、形状和异构构型在内的空间因素对毒性有很大影响。电子参数也已被证明会影响某些杀虫剂类别的生物活性,例如,以哈米特常数σ和塔夫脱常数σ*作为电负性指标。新型拟除虫菊酯类合成杀虫剂不断被开发出来,它们具有不同的结构以及不同的物理化学和生物学特性。

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