Disease relevance of 1,4-Benzodiazepine

• The present study was undertaken to investigate a novel 1,4-benzodiazepine (Bz-423) that induces apoptosis and limits autoimmune disease in NZB/NZW mice, to determine its activity against lupus-like disease associated with defective Fas expression [1].
• Bz-423 is a 1,4-benzodiazepine that suppresses disease in lupus-prone mice by selectively killing pathogenic lymphocytes, and it is less toxic compared to current lupus drugs [2].
• Patients who discontinued 1,4-benzodiazepine (n = 37) had a greater improvement in attention span, alertness, balance, drooling, and mood compared to the remainder of the group [3].
• Clonazepam is a potent anticonvulsant 1,4-benzodiazepine that controls some types of myoclonus [4].
• Testicular toxicity induced by oral administration of SC-32855, A 1,4-benzodiazepine, in the dog [5].

Psychiatry related information on 1,4-Benzodiazepine

• Loprazolam is a 1,4-benzodiazepine with hypnotic properties, advocated for use in acute or chronic insomnia [6].

High impact information on 1,4-Benzodiazepine

• The properties of a proapoptotic 1,4-benzodiazepine, Bz-423, identified through combinatorial chemistry and phenotype screening are described [7].
• Bz-423 is a novel proapoptotic 1,4-benzodiazepine that induces cell death via a superoxide signal [8].
• A series of 1,3,4-benzotriazepine-based CCK(2) antagonists have been devised by consideration of the structural features that govern CCK receptor affinity and the receptor subtype selectivity of 1,4-benzodiazepine-based CCK(2) antagonists [9].
• Clonazepam is a high-potency 1,4-benzodiazepine derivative with an intermediate to long elimination half-life that is used mainly in neurology as an antiepileptic [10].
• A 1,4-benzodiazepine analogue alprazolam (1) undergoes ring-opening hydrolysis under acidic conditions to form a triazolobenzophenone (2) [11].

Biological context of 1,4-Benzodiazepine

• Possible in vivo conversion of peptidoaminobenzophenone by enzymatic cleavage of the terminal amino acid, followed by chemical cyclization to 1,4-benzodiazepine, is also discussed [12].
• [3H]flunitrazepam has been used as a photoaffinity label for the specific, clonazepam-displaceable 1,4-benzodiazepine binding sites in sections of normal C57BL6J mouse brain and spinal cord [13].
• The pharmacokinetics of midazolam, a water soluble 1,4-benzodiazepine, has been studied in 12 patients (11 male, 1 female; age range 19-57 years) with epilepsy [14].
• The behavior of 1,4-benzodiazepine drugs in acidic media. II. Kinetics and mechanism of the acid-base equilibrium reaction of oxazolam [15].
• RO5-4864, a 1,4-benzodiazepine, has recently been shown to possess anticonvulsant, convulsant and anxiogenic properties and to inhibit Ca++-calmodulin-stimulated membrane phosphorylation [16].

Anatomical context of 1,4-Benzodiazepine

• Quantitative light-microscope autoradiography has been used to compare the specific, clonazepam-displaceable binding of [3H]flunitrazepam, a photoaffinity label for the 1,4-benzodiazepine receptor, in different regions of the brain and spinal cord of spastic mice and their unaffected littermates [17].
• We prepared various novel tricyclic 1,4-benzodiazepine derivatives as cholecystokinin (CCK) A antagonists, which were evaluated preliminarily for inhibition of 125I-CCK-8 binding to rat pancreatic membranes in vitro and inhibiting effect on CCK-8-induced inhibition of charcoal meal gastric emptying in mice [18].
• The study was intended to investigate whether metaclazepam (Talis), a new 1,4-benzodiazepine, and some of its metabolites were present in breast milk [19].
• Oxprenolol, a fat-soluble beta-adrenergic blocker, promoted as an anxiolytic agent to alleviate peripheral symptoms associated with anxiety, and lorazepam, a 1,4-benzodiazepine anxiolytic drug, may both depress central nervous system (CNS) function [20].

Associations of 1,4-Benzodiazepine with other chemical compounds

• Temazepam is a 1,4-benzodiazepine, newly marketed in the United States for the symptomatic treatment of the complaint of insomnia [21].
• Midazolam is a 1,4-benzodiazepine derivative with a unique chemical structure: depending on environmental pH, the drug can produce highly water-soluble salts (pH less than 4) or exist in lipophilic diazepine ring-closed form (pH greater than 4) [22].
• Using a 1,4-benzodiazepine core amino-functionalized at the C3 position, related tryptophanyl derivatives were synthesized as mimics of the tetrapeptide and subsequently extended N-terminally with gastrin and CCK address sequences [23].
• Benzimidazole derivatives as arginine mimetics in 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonists [24].
• An enzyme immunoassay for a metabolite of a new sleep inducer (450191-S), a ring-opened derivative of 1,4-benzodiazepine, in human serum [25].

Gene context of 1,4-Benzodiazepine

• Development of 1,4-benzodiazepine cholecystokinin type B antagonists [26].
• Recently, we reported structurally novel PDE4 inhibitors based on 1,4-benzodiazepine derivatives [27].
• 1,4-Benzodiazepine peripheral cholecystokinin (CCK-A) receptor agonists [28].
• Discovery of an imidazopyridine-containing 1,4-benzodiazepine nonpeptide vitronectin receptor (alpha v beta 3) antagonist with efficacy in a restenosis model [29].
• Analogues of Bz-423, a pro-apoptotic 1,4-benzodiazepine with potent activity in animal models of systemic lupus erythematosus and rheumatoid arthritis, have been designed, synthesized, and evaluated in cell-culture assays [30].

Analytical, diagnostic and therapeutic context of 1,4-Benzodiazepine

• The displacement of a series of 1,4-benzodiazepine (BDZ) drugs from a chiral stationary phase, based upon human serum albumin, for high performance liquid chromatography was investigated [31].
• A critical evaluation of the application of capillary electrophoresis to the detection and determination of 1,4-benzodiazepine tranquilizers in formulations and body materials [32].
• A reversed-phase high-performance liquid chromatographic (HPLC) method for the determination of four separate 1,4-benzodiazepine glucuronides in urine, plasma and bile is presented [33].
• Determination of an oxadiazole-substituted 1,4-benzodiazepine in plasma by high-performance liquid chromatography with ultraviolet detection and by a radioreceptor assay [34].
• Midazolam, the new investigational 1,4-benzodiazepine derivative with highly water-soluble salts, was studied as an anaesthesiological adjuvant in 11 patients undergoing elective caeserean section under epidural analgesia [35].

References