Receptor-like stereospecific binding of a pyrethroid insecticide to mouse brain membranes.
A heterogeneous particulate fraction of mouse brain homogenates binds NRDC 157 (3-phenoxybenzyl [1R, cis]-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate), a potent pyrethroid insecticide, stereospecifically and with high affinity. Stereospecific binding is a minor component of total binding (2.8%); the remainder of observed binding is predominantly nonspecific and unsaturable. Stereospecific binding is half-saturated at 4 X 10(-8)M and fully saturated at concentrations in excess of 1 X 10(-7)M. The stereospecific binding capacity of this preparation was 200-250 pmoles of NRDC 157 per gram equivalent of brain tissue (2.3-2.8 pmol/mg protein). This binding site may represent the neural receptor involved in the stereospecific toxic action of pyrethroids.
D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D001921:Brain / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D008024:Ligands; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D011722:Pyrethrins / Q000378:metabolism* / Q000633:toxicity; D011955:Receptors, Drug / Q000378:metabolism*; D013329:Structure-Activity Relationship
D008024:Ligands; D011722:Pyrethrins; D011955:Receptors, Drug