Psychiatry related information on Diazepine

• The acute effect of diazepine derivatives on the higher nervous activity in man [1].

High impact information on Diazepine

• In this paper, we investigate conformational preferences of the 8-substituted benzodiazepine analogues by examining structural modifications to both the exocyclic amide and the seven-membered diazepine ring and by studying the conformation of the benzodiazepine ring using molecular modeling, X-ray crystallography, and NMR [2].
• The diazepine analogues display selective binding to the dopamine D-4 and serotonin S-2A receptors similar to that of clozapine, but none has a dopamine D-4 selectivity (Ki for the dopamine D-2A receptor/Ki for the dopamine D-4 receptor) greater than that of clozapine [3].
• The results indicate that the presence of the 2'-hydroxyl and 5'-phosphate and the R stereochemistry at the C-8 position of the diazepine ring are necessary for the optimum interaction of inhibitors with yeast AMP deaminase [4].
• Addition of N,N'-dimethyldiaminoethane, -propane, and -butane gives diazepine, diazocine, and diazonine derivatives 13-15, respectively (X-ray structures of 13c, 14a, and 15a are available) [5].
• Taken together with the high cell permeability of diazepine 11 determined in CACO-2 cells, these results suggest that 1,4-diazepine-2,5-diones may be useful in the treatment of certain cancers [6].

Biological context of Diazepine

• 4. Compounds IV and V were identified by mass spectrometry as products of simultaneous aromatic hydroxylation and methoxylation of the diazepine I [7].
• Type I is an oxidative cyclization reaction producing the oxazepine derivative 1 from mex and the diazepine derivative 3 from toc [8].

Anatomical context of Diazepine

• Y-24180 ((+/-)-4-(2-chlorophenyl)-2-[2-(4-isobutylphenyl)ethyl]-6,9-dim eth yl-6H-thieno[3,2-f] [1,2,4]triazolo[4,3-a] [1,4] diazepine), an antagonist of platelet-activating factor (PAF) receptor, has already been reported to inhibit leukotriene B4 (LTB4)-induced activation of polymorphonuclear leukocytes [9].
• When evaluated for their binding affinity at the benzo diazepine receptor in bovine cortical membranes, the target compounds 8-13 displayed an affinity in the micromolar/submicromolar order [10].
• Selected 8-substituted 6,7,8,9-tetrahydro-5H-1,2,4-triazolo[4,3-a] diazepine derivatives were synthesised and tested for their action on the central nervous system [11].

Gene context of Diazepine

• A novel series of diazepine-based hydroxamic acid inhibitors of MMP-1, MMP-9, and MMP-13 were prepared and evaluated both in vitro and in vivo [12].
• The aryloxyanilide derivatives, which have been derived by opening the diazepine ring of 1, are a novel class as PBR ligands and have exhibited high and selective affinity for peripheral benzodiazepine receptors (PBRs) [13].
• Potent and selective TACE and MMP inhibitors utilizing the diazepine and thiazepine ring systems were synthesized and evaluated for biological activity in in vitro and in vivo models of TNF-alpha release [14].
• The results showed, however, that the diazepine ring present in 4 or spiroalkyl ring in 1 are important for high 5-HT1A or 5-HT2A binding affinity and selectivity of these compounds [15].
• The thienobenzodiazepine derivative etizolam (CAS 40054-69-1, 6-(o-chlorophenyl)-8-ethyl-1-methyl-4H-s-triazolo-(3,4-c)thienol(1 ,4) diazepine) is a potent anxiolytic with a pharmacological profile similar to that of classical benzodiazepines [16].

Analytical, diagnostic and therapeutic context of Diazepine

• Efficacy in the mouse collagen induced arthritis model was achieved with diazepine 20 [14].

References