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  • Title: Specific inhibition of benzodiazepine receptor binding by some N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives.
    Author: Primofiore G, Marini AM, Da Settimo F, Salvadori C, Martini C, Lucacchini A, Giannaccini G.
    Journal: Farmaco; 1990 Mar; 45(3):341-51. PubMed ID: 2166528.
    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.
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