cyclooxygenase/zápal

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Synthesis of celecoxib analogs that possess a N-hydroxypyrid-2(1H)one 5-lipoxygenase pharmacophore: biological evaluation as dual inhibitors of cyclooxygenases and 5-lipoxygenase with anti-inflammatory activity.

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A hitherto unknown class of celecoxib analogs was designed for evaluation as dual inhibitors of the 5-lipoxygenase/cyclooxygenase-2 (5-LOX/COX-2) enzymes. These compounds possess a SO(2)Me (11a), or SO(2)NH(2) (11b) COX-2 pharmacophore at the para-position of the N(1)-phenyl ring in conjunction with

Cyclooxygenase Isoform Exchange Blocks Brain-Mediated Inflammatory Symptoms.

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Cyclooxygenase-2 (COX-2) is the main source of inducible prostaglandin E2 production and mediates inflammatory symptoms including fever, loss of appetite and hyperalgesia. COX-1 is dispensable for fever, anorexia and hyperalgesia but is important for several other functions both under basal

Cerebrovascular cyclooxygenase-1 expression, regulation, and role in hypothalamic-pituitary-adrenal axis activation by inflammatory stimuli.

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Systemic injection of lipopolysaccharide (LPS) is a widely used model of immune/inflammatory challenge, which can invoke a host of CNS responses, including activation of the hypothalamic-pituitary-adrenal (HPA) axis. Inducible vascular prostaglandin E(2) (PGE(2)) synthesis by endothelial (ECs)

Arachidonic acid and nonsteroidal anti-inflammatory drugs induce conformational changes in the human prostaglandin endoperoxide H2 synthase-2 (cyclooxygenase-2).

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By using the technique of site-directed spin labeling combined with EPR spectroscopy, we have observed that binding of arachidonic acid and nonsteroidal anti-inflammatory drugs induces conformational changes in the human prostaglandin endoperoxide H(2) synthase enzyme (PGHS-2). Line shape broadening

Cyclooxygenase selectivity of non-steroid anti-inflammatory drugs in humans: ex vivo evaluation.

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We have recently described a novel assay to assess ex vivo the activity and selectivity on cyclooxygenase-1 and -2 (EC 1.14.99.1) of non-steroid anti-inflammatory drugs (NSAID) administered to rats [Br. J. Pharmacol. 126 (1999) 1824.]. Here, we have extended these studies to humans. Healthy male

Design of selective inhibitors of cyclooxygenase-2 as nonulcerogenic anti-inflammatory agents.

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The discovery of a second isoform of cyclooxygenase (cyclooxygenase-2) that is expressed in inflammatory cells and the central nervous system, but not in the gastric mucosa, offers the possibility of developing anti-inflammatory and analgesic agents that lack the gastrointestinal side effects of

Selective inhibitors of cyclooxygenase-2: a growing class of anti-inflammatory drugs.

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For about two years, selective inhibitors of cyclooxygenase-2 have been hailed as powerful additions to the armamentarium of nonsteroidal anti-inflammatory drugs (NSAIDs). Predicted by financial analysts to become among the pharmaceutical industry's greatest-ever blockbusters, two so-called coxibs

Comparison of cyclooxygenase-1 and -2 inhibitory activities of various nonsteroidal anti-inflammatory drugs using human platelets and synovial cells.

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Recent studies have shown that cyclooxygenase exists in two isozyme forms. Since differences in the pharmacological profiles of nonsteroidal anti-inflammatory drugs (NSAIDs) might be accounted for by varying degrees of selectivity for these isozymes, cyclooxygenase-1 and -2, the relative potency of

Molecular therapeutic targets in inflammation: cyclooxygenase and NF-kappaB.

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Inflammation is the host response to infection and injury. Inflammatory cells respond to foreign substances and inflammatory stimulus by producing bioactive mediators such as prostanoids, cytokines and chemokines. These mediators have complex, pleiotropic effects and interact with many cell types to

Cyclooxygenase-2 inhibitors and most traditional nonsteroidal anti-inflammatory drugs cause similar moderately increased risks of cardiovascular disease.

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Cyclooxygenase-2 inhibitors relieve pain from inflammatory conditions by decreasing the gastrointestinal side effects from traditional nonsteroidal anti-inflammatory drugs. Basic research provided plausible mechanisms and some observational epidemiological studies, case-control and cohort, indicated

[Tolerability of a selective cyclooxygenase-2-inhibitor (rofecoxib) in patients with intolerance reactions to nonsteroidal anti-inflammatory agents].

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OBJECTIVE Pseudoallergic reactions triggered by nonsteroidal anti-inflammatory drugs (NSAIDs) are common and caused by inhibition of the enzyme cyclooxygenase-1, whereas their therapeutic effects are mediated by inhibition of cyclooxygenase-2. This study analyzed the tolerability of the selective

Computer simulation of the interaction of non-steroidal anti-inflammatory drugs: indoprofen and NS398 with cyclooxygenase.

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We have applied computer simulation technique to study interaction of two anti-inflammatory drugs (NSAIDs) indoprofen and NS398 with cyclooxygenase (COX-1 and COX-2) enzymes. We have also investigated conformational flexibility of the two drugs by systematic search and simulated annealing molecular

Update on the use of cyclooxygenase-2-selective nonsteroidal anti-inflammatory drugs in horses.

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Nonsteroidal anti-inflammatory drugs work through inhibition of cyclooxygenase (COX) and are highly effective for the treatment of pain and inflammation in horses. There are 2 clinically relevant isoforms of COX. Cyclooxygenase-1 is constitutively expressed and is considered important for a variety

Imrecoxib: a novel and selective cyclooxygenase 2 inhibitor with anti-inflammatory effect.

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OBJECTIVE To investigate the inhibitory effect of imrecoxib, a synthetic compound of completely new structure, on cyclooxygenase 1 (COX-1) and 2 (COX-2) and its anti-inflammatory effect in vivo. METHODS The inhibitory effects of imrecoxib on cyclooxygenase 1 and 2 were studied using whole cell assay

Synthesis, anti-inflammatory, ulcerogenic and cyclooxygenase activities of indenopyrimidine derivatives.

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Objective of the present work was to evaluate the anti-inflammatory, ulcerogenicity and cyclooxygenase activity of indenopyrimidine derivatives. Anti-inflammatory activity of the tested compounds is investigated by carrageenan-induced rat paw edema assay. Compounds A1, A6, A7 and A12 exhibit the

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