Tricyclic heteroaromatic systems. 2-Phenyl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-one: a novel benzodiazepine receptor ligand.
The synthesis, unambiguous proof of structure and benzodiazepine receptor affinity and efficacy of 2-phenyl-1,2,4-triazolo[1,5-c][1,3]benzoxazin-5-one 1 are reported. The in vitro biological data indicate that 1 may be the lead compound of a new class of benzodiazepine antagonist-inverse agonist ligands.
Catarzi
D
D
Dipartimento di Scienze Farmaceutiche, Università di Firenze, Italy.
Cecchi
L
L
Colotta
V
V
Filacchioni
Martini
C
C
Giusti
L
L
Lucacchini
A
A
Valle
G
G
D000818:Animals; D048588:Benzoxazines; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D002417:Cattle; D018360:Crystallography, X-Ray; D005445:Flunitrazepam / Q000493:pharmacokinetics; D066298:In Vitro Techniques; D008024:Ligands; D009682:Magnetic Resonance Spectroscopy; D010078:Oxazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011963:Receptors, GABA-A / Q000187:drug effects*; D014230:Triazoles / Q000138:chemical synthesis* / Q000494:pharmacology
D048588:Benzoxazines; D008024:Ligands; D010078:Oxazines; D011963:Receptors, GABA-A; D014230:Triazoles; C087745:2-phenyl-1,2,4-triazolo(1,5-c)(1,3)benzoxazin-5-one; D005445:Flunitrazepam