Two new series od 2-arylpyrazolo[4,3-c]quinolin-3-ones (6,8-difluoro- and 7,9-dichloro-derivatives) have been synthesized and tested for their ability to displace [H-3]flunitrazepam from rat brain membranes. Several compounds possess comparable and sometimes higher affinity for central benzodiazepine receptors than that of diazepam. Some selected compounds were also tested in vivo in the anti-pentylenetetrazol test; some anticovulsant activity resulted for the 6,8-difluoroderivatives only.
Savini, L., Massarelli, P., Corti, P., Pellerano, C., Bruni, G., Romeo, M.R. (1993). Pyrazolo[4,3-c]quinolines. Synthesis and specific inhibition of benzodiazepine receptor binding. Note II. IL FARMACO, 48(12), 1675-1686.
Pyrazolo[4,3-c]quinolines. Synthesis and specific inhibition of benzodiazepine receptor binding. Note II
SAVINI, LUISA;MASSARELLI, PAOLA;CORTI, PIERO;PELLERANO, CESARE;BRUNI, GIANCARLO;
1993-01-01
Abstract
Two new series od 2-arylpyrazolo[4,3-c]quinolin-3-ones (6,8-difluoro- and 7,9-dichloro-derivatives) have been synthesized and tested for their ability to displace [H-3]flunitrazepam from rat brain membranes. Several compounds possess comparable and sometimes higher affinity for central benzodiazepine receptors than that of diazepam. Some selected compounds were also tested in vivo in the anti-pentylenetetrazol test; some anticovulsant activity resulted for the 6,8-difluoroderivatives only.
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https://hdl.handle.net/11365/402196
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