Pyrazolo[4,3-c]quinolines, synthesis and specific inhibition of benzodiazepine receptor binding. Note II.
Two new series of 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 [3H]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 anticonvulsant activity resulted for the 6,8-difluoroderivatives only.
Savini
L
L
Dipartimento Farmaco Chimico Technologico, Facoltà di Farmacia-Università, Siena, Italy.
Massarelli
P
P
Corti
P
P
Pellerano
C
C
Bruni
G
G
Romeo
M R
MR
D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D001665:Binding Sites; D001667:Binding, Competitive; D005260:Female; D005445:Flunitrazepam / Q000378:metabolism; D051379:Mice; D010433:Pentylenetetrazole / Q000037:antagonists & inhibitors; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000927:Anticonvulsants; D011720:Pyrazoles; D011804:Quinolines; D011963:Receptors, GABA-A; D005445:Flunitrazepam; D010433:Pentylenetetrazole