L. Savini et al., PYRAZOLO[4,3-C]QUINOLINES, SYNTHESIS AND SPECIFIC-INHIBITION OF BENZODIAZEPINE RECEPTOR-BINDING - NOTE-II, Il Farmaco, 48(12), 1993, pp. 1675-1686
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 the
ir ability to displace [H-3]flunitrazepam from rat brain membranes. Se
veral compounds possess comparable and sometimes higher affinity for c
entral benzodiazepine receptors than that of diazepam. Some selected c
ompounds were also tested in vivo in the anti-pentylenetetrazol test;
some anticovulsant activity resulted for the 6,8-difluoroderivatives o
nly.