Certain 1,2,3-triazole derivatives were prepared and tested for their ability to displace [3H]diazepam from bovine brain membranes. From these compounds, the quinolytriazole derivatives (14, 15, 16, 17) were clearly the most potent, while the naphthyl- and the naphthyridyl-triazoles were considerably less active. The p-nitrophenyl derivative (15) was the compound that bound with the highest affinity within the quinolyltriazole compounds class. The replacement of the p-nitrophenyl group with other substituents greatly decreased the binding activity. From a Lineweaver-Burk analysis of 11, it appears that the inhibition is competitive.
|Autori:||MARTINI C; MARRUCCI W; LUCACCHINI A; BIAGI G; LIVI O|
|Titolo:||SPECIFIC-INHIBITION OF BENZODIAZEPINE RECEPTOR-BINDING BY SOME 1,2,3-TRIAZOLE DERIVATIVES|
|Anno del prodotto:||1988|
|Digital Object Identifier (DOI):||10.1002/jps.2600771117|
|Appare nelle tipologie:||1.1 Articolo in rivista|