Interaction of tralomethrin, tralocythrin, and related pyrethroids in Na + channels of insect and mammalian neuronal cells

The neurotoxic activity of the tetrahalogenated pyrethroids, tralomethrin and tralocythrin, which are dibromo adducts of deltamethrin and RU 24501, respectively, and RU 27218, which is a dichloro adduct of RU 24501, have been studied on two different excitable membranes using in vitro methods: insec...

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Published inPesticide biochemistry and physiology Vol. 24; no. 3; pp. 306 - 316
Main Authors Roche, Michel, Frelin, Christian, Bruneau, Pierre, Meinard, Colette
Format Journal Article
LanguageEnglish
Published San Diego, CA Elsevier Inc 01.01.1985
Elsevier
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Summary:The neurotoxic activity of the tetrahalogenated pyrethroids, tralomethrin and tralocythrin, which are dibromo adducts of deltamethrin and RU 24501, respectively, and RU 27218, which is a dichloro adduct of RU 24501, have been studied on two different excitable membranes using in vitro methods: insect axonal membranes and mammalian neuroblastoma cells in culture. The results show that molecules whose chrysanthemic acid chain at C 3 is saturated by halogen addition have intrinsic toxicity on the sodium channels of nerve membranes. They increase the amplitude of negative after-potential, depolarize the cockroach axonal membrane, and stabilize an open conformation of voltage-dependent Na + channels in mouse neuroblastoma cells, thereby producing a massive uptakeof Na + by the cells. All effects were observed in the absence of metabolic transformation of the compounds tested. In light of these experiments, it is concluded that tralomethrin and tralocythrin cannot be considered as propyrethroids.
Bibliography:H10
874824788
ISSN:0048-3575
1095-9939
DOI:10.1016/0048-3575(85)90141-5