Pyrazolo [4,3-c] quinolines synthesis and specific inhibition of benzodiazepine receptor binding (Note I).
A series of 2-arylpyrazolo[4,3-c] quinolin-3-one derivatives, bearing different substituents in the two aromatic rings, were prepared and tested for their ability to displace [3H] flunitrazepam from rat brain membranes. Some compounds have shown an affinity for receptors comparable and sometimes higher than that of CGS series.
Dipartimento Farmaco Chimico Technologico - Università, Siena, Italy.
L
L
Savini
P
P
Massarelli
C
C
Pellerano
I
I
Fiorini
G
G
Bruni
M R
MR
Romeo
D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000378:metabolism; D005445:Flunitrazepam / Q000378:metabolism; D058787:GABA-A Receptor Antagonists; D066298:In Vitro Techniques; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism
D058787:GABA-A Receptor Antagonists; D011720:Pyrazoles; D011804:Quinolines; D005445:Flunitrazepam