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非神经机制对拟除虫菊酯构效关系的影响。

Effects of non-neural mechanisms on pyrethroid structure-activity relationships.

作者信息

Soderlund D M

出版信息

J Environ Sci Health B. 1983;18(1):15-27. doi: 10.1080/03601238309372356.

DOI:10.1080/03601238309372356
PMID:6833714
Abstract

Structural requirements for high insecticidal activity in pyrethroid insecticides are very stringent. Observed structure-activity relationships may arise either from specificity at the site of pyrethroid action in the nervous system, from selectivity in the pharmacokinetic processes governing the appearance and persistence of compounds at that site, or from a combination of these mechanisms. Recent studies of the metabolism of trans and cis isomers of pyrethroids in insect tissue preparations in vitro and of their pharmacokinetic behavior in insects in vivo permit an assessment of the impact of non-neural mechanisms on the toxicity differences observed between these isomers.

摘要

拟除虫菊酯类杀虫剂具有高杀虫活性的结构要求非常严格。观察到的构效关系可能源于拟除虫菊酯在神经系统作用位点的特异性,源于控制化合物在该位点出现和持续存在的药代动力学过程中的选择性,或者源于这些机制的组合。最近对拟除虫菊酯的反式和顺式异构体在昆虫组织体外制剂中的代谢及其在昆虫体内的药代动力学行为的研究,使得人们能够评估非神经机制对这些异构体之间观察到的毒性差异的影响。

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