Article date: 1987/2/1
PubMed ID: 3029901
Journal name: Toxicology letters (ISSN: 0378-4274)
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 microM. Type II pyrethroids inhibited [35S]TBPS binding to rat brain synaptosomes with Ki values ranging from 5-10 microM. The data presented here suggest that the interaction of Type II pyrethroids with the gamma-aminobutyric acid (GABA) receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site.
Author List: Crofton K M, Reiter L W, Mailman R B
Publication Types: Journal Article
Substances mentioned in the article: Bridged Bicyclo Compounds; Bridged Bicyclo Compounds, Heterocyclic; Nitriles; Pyrethrins; Receptors, GABA-A; cypermethrin; Muscimol; decamethrin; cismethrin; Permethrin; Flunitrazepam; tert-butylbicyclophosphorothionate; Diazepam; fenvalerate;
Mesh terms: Animals; Binding, Competitive; Brain/metabolism; Bridged Bicyclo Compounds/metabolism; Bridged Bicyclo Compounds, Heterocyclic; Diazepam/metabolism; Flunitrazepam/metabolism; Male; Muscimol/metabolism; Nitriles; Permethrin; Pyrethrins/metabolism; Rats; Receptors, GABA-A/metabolism;