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Evidence that 2 phenylpyrazolo 4 3 c quinolin 3 5h one antagonizes pharmacological electrophysiological and biochemical effects of diazepam in rats


, : Evidence that 2 phenylpyrazolo 4 3 c quinolin 3 5h one antagonizes pharmacological electrophysiological and biochemical effects of diazepam in rats. Neuropharmacology 24(2): 99-106

The effects of the acute administration of 2-phenylpyrazolo[4,3-c]quinolin-3(5H)-one on diazepam-induced behavior and electrophysiological activity were studied in rat. The compound, in doses of 5-10 mg/kg (i.p.), which per se did not induce alterations in spontaneous locomotor activity, antagonized the sedative effective induced by 5-10 mg/kg (i.p.) of diazepam. The injection of diazepam in rats, induced a profound reduction in the 1st negative wave of the recording of the visual evoked potential used as a sensitive electrophysiological test, in vivo. 2-Phenylpyrazolo[4,3-c]quinolin-3(5H)-one (10 mg/kg, i.p.) caused a recovery of the amplitude of the 1st negative wave within a few minutes. 2-Phenylpyrazolo[4,3-c]quinolin-3(5H)-one, injected acutely in rats, pre-treated with diazepam exhibited the capacity to antagonize the binding of [3H]diazepam determined in vitro on synaptic membrane preparations from cortex. The comparison of the pattern of the visual-evoked potential, recorded after the injection of 2-phenylpyrazolo[4,3-c]quinolin-3(5H)-one (50 mg/kg) with the patterns recorded after the injection of ethyl-8-fluoro-5,6-dihydro-5-methyl-6-oxo-4H-imidazolo(1,5a)-(1,4)benzodiazepine-3-carboxylate (50 mg/kg) and ethyl-.beta.-carboline-3-carboxylate and 1-methyl-.beta.-carboline demonstrated that 2-phenylpyrazolo[4,3-c]quinolin-3(5H)-one is devoid of intrinsic activity.

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