Several optically active N-(indol-3-ylglyocylyl)amino acid derivatives were synthesized and tested for [3H]flunitrazepam displacing activity in bovine brain membranes. IC50 values were measured and revealed that the D form of the amino acid moiety of the compounds was more potent than both the L form and racemic form, suggesting a key role of the amino acid stereochemistry on the affinity to the benzodiazepine receptors. GABA ratio and proconvulsant/convulsant data reported for the most active compounds reveal they behave as inverse agonists at the benzodiazepine receptor.
|Autori interni:||MARINI, ANNA MARIA|
DA SETTIMO PASSETTI, FEDERICO
|Autori:||Primofiore G; Marini AM; Da Settimo F; Martini C; Bardellini A; Giannaccini G; Lucacchini A.|
|Titolo:||SPECIFIC-INHIBITION OF BENZODIAZEPINE RECEPTOR-BINDING BY SOME N-(INDOL-3-YLGLYOXYLYL)AMINO ACID-DERIVATIVES - STEREOSELECTIVE INTERACTIONS|
|Anno del prodotto:||1989|
|Digital Object Identifier (DOI):||10.1021/jm00132a004|
|Appare nelle tipologie:||1.1 Articolo in rivista|