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Non-erythroid alpha-spectrin breakdown by calpain and interleukin 1 beta-converting-enzyme-like protease(s) in apoptotic cells: contributory roles of both protease families in neuronal apoptosis.
The results suggest that both protease families participate in the expression of neuronal apoptosis, and inhibition of either ICE-like protease(s) or calpain protects both granule neurons and SH-SY5Y cells against apoptosis. Expand
Lack of beneficial effect of COX-2 inhibitors in an experimental model of colitis.
The data show that despite their potent extraintestinal antiinflammatory activity, COX-2 inhibitors do not seem to have any beneficial effect in TNBS colitis and raise the question whether this therapeutic approach would be beneficial in patients with IBD. Expand
Effects of novel anti-inflammatory compounds on healing of acetic acid-induced gastric ulcer in rats.
Derivatives of 2,6-di-tert-butylphenol, whose members may act as PGHS-1/PGHS-2 inhibitors or PGHS/5-LO dual inhibitors, are novel anti-inflammatory compounds that are devoid of GI irritating effects and do not affect the rate of pre-existing gastric ulcer healing. Expand
Synthesis, structure-activity relationships, and pharmacological profile of 9-amino-4-oxo-1-phenyl-3,4,6,7-tetrahydro[1,4]diazepino[6, 7,1-hi]indoles: discovery of potent, selective phosphodiesterase
The synthesis, structure-activity relationships, and biological properties of a novel series of potent and selective phosphodiesterase type 4 (PDE4) inhibitors are described and one compound was found to exhibit potent in vivo activity in antigen-induced eosinophil recruitment in Brown-Norway rats and in production of TNFalpha in Wistar rats. Expand
Characterization of CPP32‐Like Protease Activity Following Apoptotic Challenge in SH‐SY5Y Neuroblastoma Cells
The activation of interleukin‐1β‐converting enzyme (ICE)‐like proteases (caspases) in human neuroblastoma cells (SH‐SY5Y) following challenge with staurosporine, an established agent known to induce apoptosis is characterized. Expand
Synthesis, Structure−Activity Relationships, and in Vivo Evaluations of Substituted Di-tert-butylphenols as a Novel Class of Potent, Selective, and Orally Active Cyclooxygenase-2 Inhibitors. 1.
Selective cyclooxygenase-2 (COX-2) inhibitors have been shown to be potent antiinflammatory agents with fewer side effects than currently marketed nonsteroidal antiinflammatory drugs (NSAIDs).Expand
Comparative in vitro and in vivo activities of two 9-deazaguanine analog inhibitors of purine nucleoside phosphorylase, CI-972 and PD 141955.
An in-parallel comparison is presented of the in vitro and in vivo properties of two 9-deazaguanine analog inhibitors of purine nucleoside phosphorylase (PNP) and PD 141955, with PD considerably more potent and active in all systems studied. Expand
The antiinflammatory effects of adenosine receptor agonists on the carrageenan-induced pleural inflammatory response in rats.
In mechanistic studies, R-N-(1-methyl-2-phenylethyl)adenosine, a standard A1 selective agonist, reversed the drop in circulating neutrophil count that occurs after injection of carrageenan, indicating that adenosine receptor agonists are effective new pharmacologic tools for the study of inflammatory processes. Expand
The role of neutrophils in type II collagen-induced arthritis in rats.
In rats depleted of neutrophils with rabbit anti-rat neutrophil antiserum (ANS), swelling and inflammation associated with the arthritis response were maximally reduced by 65% (P less than 0.001). Expand
Inhibitors of human purine nucleoside phosphorylase. Synthesis and biological activities of 8-amino-3-benzylhypoxanthine and related analogues.
2,8-Diamino-3-substituted hypoxanthines (16a-d) represent a novel structural type hitherto unreported in the literature, and efficient methodologies for their synthesis were developed in the present studies. Expand