Several N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives were synthesized and tested for their affinity for the benzodiazepine receptor in bovine cortical membranes. The 2-methyl derivatives showed a lower affinity than the unmethylated analogues, and the 1,2-dimethyl derivatives practically lacked any affinity for the benzodiazepine receptor. The importance of the indole N-H group is therefore evidenced for an optimal interaction of these ligands with receptor site.
SPECIFIC-INHIBITION OF BENZODIAZEPINE RECEPTOR-BINDING BY SOME N-(2-METHYL OR 1,2-DIMETHYLINDOL-3-YLGLYOXYLYL)AMINO ACID-DERIVATIVES.
MARINI, ANNA MARIA;DA SETTIMO PASSETTI, FEDERICO;MARTINI, CLAUDIA;LUCACCHINI, ANTONIO;GIANNACCINI, GINO
1990-01-01
Abstract
Several N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives were synthesized and tested for their affinity for the benzodiazepine receptor in bovine cortical membranes. The 2-methyl derivatives showed a lower affinity than the unmethylated analogues, and the 1,2-dimethyl derivatives practically lacked any affinity for the benzodiazepine receptor. The importance of the indole N-H group is therefore evidenced for an optimal interaction of these ligands with receptor site.File in questo prodotto:
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