| 7682602 |
Sola C, Martinez E, Camon L, Pazos A, Rodriguez-Farre E: Lindane administration to the rat induces modifications in the regional cerebral binding of [3H] Muscimol, [3H]-flunitrazepam, and t-[35S] butylbicyclophosphorothionate: an autoradiographic study. J Neurochem. 1993 May;60(5):1821-34.
The effect of lindane administration on the specific binding of ligands to different sites on the GABAA receptor-ionophore complex was studied in the rat brain by receptor mapping autoradiography. [3H] Muscimol (Mus), [3H] flunitrazepam (Flu), and t-[35S] butylbicyclophosphorothionate (TBPS) were used as specific ligands of GABA, benzodiazepine, and picrotoxinin binding sites, respectively. Rats received a single oral dose of 30 mg/kg lindane and they were classified into two groups according to the absence or presence of convulsions. Vehicle-treated groups acted as controls. The effect of the xenobiotic on ligand binding was measured in different brain areas and nuclei 12 min or 5 h after its administration. Lindane induced a generalized decrease in [35S] TBPS binding, which was present shortly after dosing. In addition, [3H] Flu binding was increased in lindane-treated animals, this modification also appearing shortly after administration but diminishing during the studied time. Finally, lindane induced a decrease in [3H] Mus binding, which became more evident over time. These modifications were observed both in the presence and in the absence of convulsions. However, an increase in [3H]-Mus binding was detected shortly after lindane-induced convulsions. The observed decrease in [35S] TBPS binding is in agreement with the postulated action of lindane at the picrotoxinin binding site of the GABAA receptor chloride channel. The effects observed on the binding of [3H] Flu and [3H] Mus may be secondary to the action of lindane as an allosteric antagonist of the GABAA receptor. |
81(1,1,1,1) |