反应详情

Dose-response displacement assays were conducted using 2-methyl carboxylate-5,7-dichloro-4-[[(diphenylamino)-carbonyl]amino]-quinoline and [3H]-TCP (both with and without added glycine), and [3H]-muscimol. Displacement of [3H]-TCP binding was assayed in the presence of 10 uM L-glutamic acid and 3 uM glycine. This assay was conducted twice with triplicate samples and concentrations of test compound ranging from 1 uM to 5 nM. No significant effect on [3H]-TCP binding was observed in this assay. Repetition of the TCP displacement experiment with L-glutamate but no added glycine gave similar results over a dose range of 5 uM to 10 nM. A synaptosomal competition binding assay was also conducted using 2-methyl carboxylate-5,7-dichloro-4-[[(diphenylamino)-carbonyl]amino]-quinoline and the ligand [3H]-muscimol. The purpose of this experiment was to check for activity at the GABA-A receptor complex. No significant effects were observed. The compound 2-methyl carboxylate-5,7-dichloro-4-[[(diphenylamino)-carbonyl]anino]-quinoline also tested negative for PCP activity at the NMDA receptor, and for GABA-A effects.