Pyrethroid insecticides and radioligand displacement from the GABA receptor chloride ionophore complex
Radioligand binding displacement studies were conducted to determine the effects of Type I and II pyrethroids on /sup 3/H-flunitrazepam (FLU), /sup 3/H-muscimol (MUS), and (/sup 35/S-t-butylbicyclophosphorothionate (TBPS) binding. Competition experiments with /sup 3/H-FLU and /sup 3/H-MUS indicate a lack of competition for binding by the pyrethroids. Type I pyrethroids failed to compete for the binding of (/sup 35/S-TBPS at concentrations as high as 50 pM. Type II pyrethroids inhibited (/sup 35/S-TBPS binding to rat brain synaptosomes with Ki values ranging from 5-10 pM. The data presented suggest that the interaction of Type II pyrethroids with the GABA receptor-ionophore complex is restricted to a site near the TBPS/picrotoxinin binding site.
- Research Organization:
- Environmental Protection Agency, Research Triangle Park, NC (USA). Health Effects Research Lab.
- OSTI ID:
- 6375624
- Report Number(s):
- PB-87-212445/XAB; EPA-600/J-87/050
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOCHEMICAL REACTION KINETICS
BODY
ENDOCRINE GLANDS
GLANDS
HAZARDOUS MATERIALS
HYDROGEN ISOTOPES
INSECTICIDES
ISOTOPE APPLICATIONS
ISOTOPES
KINETICS
LIGANDS
LIGHT NUCLEI
MAMMALS
MATERIALS
NUCLEI
ODD-EVEN NUCLEI
ORGANS
PARATHYROID GLANDS
PESTICIDES
RADIOISOTOPES
RATS
REACTION KINETICS
RODENTS
TRACER TECHNIQUES
TRITIUM
VERTEBRATES
YEARS LIVING RADIOISOTOPES