PK 11195 antagonism of pyrethroid-induced proconvulsant activity

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

Research output: Contribution to journalArticle

27 Citations (Scopus)

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
StatePublished - Feb 18 1986
Externally publishedYes

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Pyrethrins
Permethrin
Pentylenetetrazole
fenvalerate
Benzodiazepines
Seizures
Binding Sites
Phenytoin
PK 11195
cypermethrin
decamethrin

All Science Journal Classification (ASJC) codes

  • Cellular and Molecular Neuroscience
  • Pharmacology

Cite this

PK 11195 antagonism of pyrethroid-induced proconvulsant activity. / Devaud, Leslie L.; Szot, Patricia; Murray, Thomas F.

In: European Journal of Pharmacology, Vol. 121, No. 2, 18.02.1986, p. 269-273.

Research output: Contribution to journalArticle

Devaud, Leslie L. ; Szot, Patricia ; Murray, Thomas F. / PK 11195 antagonism of pyrethroid-induced proconvulsant activity. In: European Journal of Pharmacology. 1986 ; Vol. 121, No. 2. pp. 269-273.
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