1,3-Diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones. 4. Synthesis and specific inhibition of benzodiazepine receptor binding.
A series of 1,3-diarylpyrazolo[4,5-c]- and -[5,4-c]quinolin-4-ones were prepared and tested for their ability to displace [3H]flunitrazepam from bovine brain membranes. While the 1,3-diarylpyrazolo[4,5-c]quinoline derivatives showed affinity for the receptor site, their [5,4-c] isomers were devoid of binding activity.
Palazzino
G
G
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Cecchi
L
L
Melani
F
F
Colotta
V
V
Filacchioni
G
G
Martini
C
C
Lucacchini
A
A
D000818:Animals; D001667:Binding, Competitive; D001921:Brain / Q000378:metabolism; D002417:Cattle; D005445:Flunitrazepam / Q000378:metabolism; D007536:Isomerism; D009682:Magnetic Resonance Spectroscopy; D008566:Membranes / Q000378:metabolism; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000378:metabolism*; D013329:Structure-Activity Relationship
D011720:Pyrazoles; D011804:Quinolines; D011963:Receptors, GABA-A; D005445:Flunitrazepam