The Experts below are selected from a list of 96 Experts worldwide ranked by ideXlab platform
B M Peskar - One of the best experts on this subject based on the ideXlab platform.
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aspirin like drugs may block pain independently of Prostaglandin Synthesis inhibition
Cellular and Molecular Life Sciences, 1991Co-Authors: Kay Brune, W S Beck, Gerd Geisslinger, S Menzelsoglowek, B M PeskarAbstract:Using flurbiprofen, a chiral anti-inflammatory and analgesic 2-arylpropionic acid derivative, the enantiomers of which are not converted to each other (less than 5%) in rats or man, we obtained evidence that Prostaglandin Synthesis inhibition is primarily mediating the anti-inflammatory activity but Prostaglandin Synthesis independent mechanisms contribute to the analgesic effects. Thus, the S-form inhibited Prostaglandin Synthesis, inflammation and nociception in rats. The R-form had much less effect on Prostaglandin Synthesis and did not affect inflammation. It did, however, block nociception in rats almost as potently as the S-form. S-flurbiprofen, in contrast to the R-form, was clearly ulcerogenic in the gastrointestinal mucosa. These results indicate additional molecular mechanisms of analgesia and suggest the use of R-arylpropionic acids as analgesics.
Johannes Van Staden - One of the best experts on this subject based on the ideXlab platform.
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screening of zulu medicinal plants for Prostaglandin Synthesis inhibitors
Journal of Ethnopharmacology, 1996Co-Authors: A K Jager, Anne Hutchings, Johannes Van StadenAbstract:Aqueous and ethanolic extracts of 39 plants used in traditional Zulu medicine to treat headache or inflammatory diseases were screened for Prostaglandin-Synthesis inhibitors. Extracts were tested in an in vitro assay for cyclooxygenase inhibitors. In general, ethanolic extracts caused higher inhibition than aqueous extracts. Two-thirds of the plants screened had high inhibitory activity. The highest inhibition was obtained with ethanolic extracts of Bidens pilosa, Eucomis autumnalis, Harpephyllum caffrum, Helichrysum nudifolium, Leonotis intermedia, L. leonorus, Ocotea bullata, Rumex saggitatus, Solanum mauritianum, Synadenium cupulare and Trichilia dregeana.
Juan C Leza - One of the best experts on this subject based on the ideXlab platform.
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stress mediators regulate brain Prostaglandin Synthesis and peroxisome proliferator activated receptor γ activation after stress in rats
Endocrinology, 2008Co-Authors: Borja Garciabueno, Jose L M Madrigal, Beatriz G Pereznievas, Juan C LezaAbstract:Stress exposure leads to oxidative/nitrosative and neuroinflammatory changes that have been shown to be regulated by antiinflammatory pathways in the brain. In particular, acute restraint stress is followed by cyclooxygenase (COX)-2 up-regulation and subsequent proinflammatory Prostaglandin (PG) E2 release in rat brain cortex. Concomitantly, the Synthesis of the antiinflammatory Prostaglandin 15d-PGJ2 and the activation of its nuclear target the peroxisome proliferator-activated receptor (PPAR)-γ are also produced. This study aimed to determine the possible role of the main stress mediators: catecholamines, glucocorticoids, and excitatory amino acids (glutamate) in the above-mentioned stress-related effects. By using specific pharmacological tools, our results show that the main mediators of the stress response are implicated in the regulation of Prostaglandin Synthesis and PPARγ activation in rat brain cortex described after acute restraint stress exposure. Pharmacological inhibition (predominantly throu...
Regina M Botting - One of the best experts on this subject based on the ideXlab platform.
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cyclooxygenase isozymes the biology of Prostaglandin Synthesis and inhibition
Pharmacological Reviews, 2004Co-Authors: Daniel L Simmons, Regina M BottingAbstract:Nonsteroidal anti-inflammatory drugs (NSAIDs) represent one of the most highly utilized classes of pharmaceutical agents in medicine. All NSAIDs act through inhibiting Prostaglandin Synthesis, a catalytic activity possessed by two distinct cyclooxygenase (COX) isozymes encoded by separate genes. The discovery of COX-2 launched a new era in NSAID pharmacology, resulting in the Synthesis, marketing, and widespread use of COX-2 selective drugs. These pharmaceutical agents have quickly become established as important therapeutic medications with potentially fewer side effects than traditional NSAIDs. Additionally, characterization of the two COX isozymes is allowing the discrimination of the roles each play in physiological processes such as homeostatic maintenance of the gastrointestinal tract, renal function, blood clotting, embryonic implantation, parturition, pain, and fever. Of particular importance has been the investigation of COX-1 and -2 isozymic functions in cancer, dysregulation of inflammation, and Alzheimer's disease. More recently, additional heterogeneity in COX-related proteins has been described, with the finding of variants of COX-1 and COX-2 enzymes. These variants may function in tissue-specific physiological and pathophysiological processes and may represent important new targets for drug therapy.
Kay Brune - One of the best experts on this subject based on the ideXlab platform.
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aspirin like drugs may block pain independently of Prostaglandin Synthesis inhibition
Cellular and Molecular Life Sciences, 1991Co-Authors: Kay Brune, W S Beck, Gerd Geisslinger, S Menzelsoglowek, B M PeskarAbstract:Using flurbiprofen, a chiral anti-inflammatory and analgesic 2-arylpropionic acid derivative, the enantiomers of which are not converted to each other (less than 5%) in rats or man, we obtained evidence that Prostaglandin Synthesis inhibition is primarily mediating the anti-inflammatory activity but Prostaglandin Synthesis independent mechanisms contribute to the analgesic effects. Thus, the S-form inhibited Prostaglandin Synthesis, inflammation and nociception in rats. The R-form had much less effect on Prostaglandin Synthesis and did not affect inflammation. It did, however, block nociception in rats almost as potently as the S-form. S-flurbiprofen, in contrast to the R-form, was clearly ulcerogenic in the gastrointestinal mucosa. These results indicate additional molecular mechanisms of analgesia and suggest the use of R-arylpropionic acids as analgesics.
