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Lummis SC, Chow SC, Holan G, Johnston GA: gamma-Aminobutyric acid receptor ionophore complexes: differential effects of deltamethrin, dichlorodiphenyltrichloroethane, and some novel insecticides in a rat brain membrane preparation. J Neurochem. 1987 Mar;48(3):689-94. The binding of [35S] t-butylbicyclophosphorothionate ([35S] TBPS), a gamma-aminobutyric acid (GABA)-activated chloride ionophore ligand; [3H] diazepam, a benzodiazepine agonist; and [3H] muscimol, a GABA receptor probe, were used to assess the effects at 100 microM of deltamethrin, dichlorodiphenyltrichloroethane (DDT), and three experimental insecticides--a DDT-pyrethroid hybrid, GH414 (cycloprothrin), and two DDT-analogues, GH266 and GH149 (EDO), on GABA receptor ionophore complexes in a rat brain membrane preparation. GH266 and GH149 were found to inhibit a greater percentage of [35S] TBPS binding than the same concentration of deltamethrin or DDT, although GH414 had little effect. GH266 and GH149 enhanced [3H] diazepam binding by nearly 200%, in contrast to the inhibitory effects of deltamethrin, DDT, and GH414. GH266 and GH149 also caused a dramatic enhancement of [3H] muscimol binding, 367 and 236% of control, respectively, whereas DDT and deltamethrin caused only a moderate enhancement. The effects of the insecticides on binding affinity and density were examined for each of the ligands. The results show a differential interaction of the insecticides on the various ligand binding sites. |
112(1,2,2,2) |