Pyrethroid insecticides and radioligand displacement from the gaba receptor chloride ionophore complex

Kevin M. Crofton, Lawrence W. Reiter, Richard Mailman

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Abstract

Radioligand binding displacement studies were conducted to determine the effects of Type I and II pyrethroids on [3H]flunitrazepam (FLU), [3H]muscimol (MUS), and [35S]t-butylbicyclophosphorothionate (TBPS) binding. Competition experiments with [3H]FLU and [3H]MUS indicate a lack of competition for binding by the pyrethroids. Type I pyrethroids failed to compete for the binding of [35S]TBPS at concentrations as high as 50 μM. Type II pyrethroids inhibited [35S]TBPS binding to rat brain synaptosomes with Ki, values ranging from 5-10 μM. The data presented here suggest that the interaction of Type II pyrethroids with the γ-aminobutyric acid (GABA) receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site.

Original languageEnglish (US)
Pages (from-to)183-190
Number of pages8
JournalToxicology Letters
Volume35
Issue number2-3
DOIs
StatePublished - Jan 1 1987

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All Science Journal Classification (ASJC) codes

  • Toxicology

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