Certain 1,2,3-triazole derivatives were prepared and tested for their ability to displace [3H]diazepam that was bound to bovine brain membrane protein. All the tested compounds are essentially lacking in this ability, except for B.1, which inhibited binding of [3H]diazepam in 50% of the trials at 2.5 microM. The structure of B.1, with a 1,2,3-triazole ring with acidic properties, supports the hypothesis proposed for binding to the benzodiazepine receptor site. Comparison of B.1 with 1,2,3-triazole derivatives bearing a bicyclic substituent in position 1 of the heterocyclic ring suggests that a high steric hindrance increases the affinity of a compound for the benzodiazepine receptor.
|Autori:||BIAGI G; LIVI O; LUCACCHINI A; MARTINI C; SCARTONI V|
|Titolo:||Specific inhibition of binding to benzodiazepine receptors by 1,2,3-triazole derivatives.|
|Anno del prodotto:||1992|
|Digital Object Identifier (DOI):||10.1002/jps.2600810615|
|Appare nelle tipologie:||1.1 Articolo in rivista|