PK 11195 antagonism of pyrethroid-induced proconvulsant activity

Leslie L. Devaud, Patricia Szot, Thomas F. Murray

Research output: Contribution to journalArticle

27 Scopus citations

Abstract

The acute administration of 1R,cis,αS-cypermethrin, deltamethrin fenvalerate and permethrin produced a dose-dependent lowering of the dose of pentylenetetrazol required to elicit a seizure in rats. The proconvulsant action of cypermethrin displayed stereospecificity in that the 1R,cis,αS isomer of cypermethrin was the most potent compound tested, while the non-insecticidal isomer, 1S,cis,αR-cypermethrin, was devoid of proconvulsant activity. Pretreatment of rats with PK 11195, an antagonist of the peripheral-type benzodiazepine binding site, elicited a complete reversal of the proconvulsant actions of both deltamethrin and permethrin. In contrast, pretreatment with phenytoin did not alter the pyrethroid-induced proconvulsant activity. These results suggest that the effect of pyrethroids on pentylenetetrazol seizure threshold are mediated via an interaction with peripheral-type benzodiazepine binding sites.

Original languageEnglish
Pages (from-to)269-273
Number of pages5
JournalEuropean Journal of Pharmacology
Volume121
Issue number2
DOIs
Publication statusPublished - Feb 18 1986
Externally publishedYes

    Fingerprint

All Science Journal Classification (ASJC) codes

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this