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

  • Kevin M. Crofton, Lawrence W. Reiter, Richard B. Mailman
  • Toxicology Letters, February 1987, Elsevier
  • DOI: 10.1016/0378-4274(87)90205-0

Pyrethroids Bind to GABA receptor

What is it about?

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.

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