title: Specific inhibition of benzodiazepine receptor binding by some N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives.
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.
authors.affiliation: Istituto di Chimica Farmaceutica dell'Università di Pisa, Italy.
authors.forename: G
authors.initials: G
authors.lastname: Primofiore
authors.forename: A M
authors.initials: AM
authors.lastname: Marini
authors.forename: F
authors.initials: F
authors.lastname: Da Settimo
authors.forename: C
authors.initials: C
authors.lastname: Salvadori
authors.forename: C
authors.initials: C
authors.lastname: Martini
authors.forename: A
authors.initials: A
authors.lastname: Lucacchini
authors.forename: G
authors.initials: G
authors.lastname: Giannaccini
mesh_terms: D000596:Amino Acids / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D001667:Binding, Competitive / Q000187:drug effects; D002417:Cattle; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism; D055598:Chemical Phenomena; D002621:Chemistry; D005445:Flunitrazepam / Q000378:metabolism; D006038:Glyoxylates / Q000138:chemical synthesis / Q000494:pharmacology; D066298:In Vitro Techniques; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D009682:Magnetic Resonance Spectroscopy; D008566:Membranes / Q000187:drug effects / Q000378:metabolism; D011963:Receptors, GABA-A / Q000187:drug effects* / Q000378:metabolism; D013055:Spectrophotometry, Infrared
chemical_list: D000596:Amino Acids; D006038:Glyoxylates; D007211:Indoles; D011963:Receptors, GABA-A; D005445:Flunitrazepam