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.
SPECIFIC-INHIBITION OF BENZODIAZEPINE RECEPTOR-BINDING BY SOME N-(INDOL-3-YLGLYOXYLYL)AMINO ACID-DERIVATIVES - STEREOSELECTIVE INTERACTIONS
MARINI, ANNA MARIA;DA SETTIMO PASSETTI, FEDERICO;MARTINI, CLAUDIA;GIANNACCINI, GINO;LUCACCHINI, ANTONIO
1989-01-01
Abstract
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.File in questo prodotto:
Non ci sono file associati a questo prodotto.
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
