1,5-Benzodiazepine tricyclic derivatives exerting anti-inflammatory effects in mice by inhibiting interleukin-6 and prostaglandinE2production

γ-Aminbuturic Acid A Receptor Mitigates Homocysteine-Induced Endothelial Cell Permeability

“…Along with extracellular matrix (ECM) degradation, tissue plasminogen activator causes proteolytic shedding of γ-aminobutyric acid (GABA) receptors (Mataga et al 2002;Frey et al 1996). GABA receptors play a significant role in brain microvascular permeability, which if inhibited, alters the neuronal environment and leads to ECM degradation and edema (Lee et al 1995;Limmroth et al 1996;Fruscella et al 2001;Lazzarini et al 2001). Hcy competes with GABA receptors and acts as an excitatory neurotransmitter.…”

Anti-inflammatory Effects of Diazepam on Different Models of Inflammation: Roles ofPeripheral Benzodiazepine Receptors and Genes for Corticosterone, Nitric Oxide andCytokines Biosynthesis

“…Also, it is consistent with results of Righi et al [23], who reported that diazepam treatment (3 mg/kg I.P) daily for 30 days produced a significant increase in the serum corticosterone levels in the treated hamsters in relation to those measured in the animals of control saline treated group. Also, from the results of chronic inflammatory study, revealed that diazepam significantly increased serum albumin level and decreasing significantly serum C-reactive protein, which is an acute phase protein commonly used to assess the disease activity in the inflammatory rheumatic diseases, and this effect of diazepam could be explained by the fact that it can suppress secretion of pro-inflammatory cytokines from mouse macrophages such as TNF-α, IL-1, and IL-6 which is the main stimulator of acute phase protein synthesis during acute and chronic inflammation [9,21,24]. Bilateral adrenalectomized were done in some rat groups of acute and chronic inflammatory studies of the present work to show that the anti-inflammatory effects of diazepam were due to stimulation of genes responsible for endogenous corticosterone secretion from the adrenal glands, where the adrenalectomy significantly precluded and prevented the anti-inflammatory effects attributed to diazepam on CIPE in rats, also on the adjuvant arthritic rats as was demonstrated by the inability of diazepam to affect the different arthritic parameters of the adrenalectomized arthritic rats.…”

A Convenient Method for the Synthesis of 1,5-benzodiazepin-2-one

“…These beneficial health properties have led to several investigations on their chemical structures and have initiated a number of synthetic efforts to access 1,5-benzodiazepine derivatives [15,[19][20][21][22][23][24][25][26][27][28]. In this work, we describe a new method for the synthesis of 3-hydroxy-1,5-benzodiazepin-2-ones based on the condensation of o-phenylenediamines with a cis and trans ethyl 3-phenylglycidate.…”