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  • inhibition
  • However, with regard to this drug's promise for the therapy of advanced cancers, it is unclear whether the inhibition of COX-2 plays a dominant role, and this has become a controversial and intensely researched issue. (wikipedia.org)
  • However, when the ability of all these compounds to kill tumor cells in cell culture was investigated, it turned out that the antitumor potency did not at all depend on whether or not the respective compound could inhibit COX-2, showing that inhibition of COX-2 was not required for the anticancer effects. (wikipedia.org)
  • These drugs have at least a 200- to 300-fold selectivity for inhibition of COX-2 over COX-1. (uptodate.com)
  • Like its ability to control pain, aspirin's ability to control fever is due to its action on the prostaglandin system through its irreversible inhibition of COX. (wikipedia.org)
  • selectivity
  • Structure activity relationship (SAR) studies for diaryl heterocyclic compounds have indicated that a cis-stilbene moiety and changes in the para-position of one of the aryl rings play an important role in COX-2 selectivity. (wikipedia.org)
  • analgesic
  • COX-2 inhibitors are important drugs with analgesic and anti-inflammatory effects. (booktopia.com.au)
  • Significant pain relief occurred within 2 days of the initiation of treatment, and maximum anti-inflammatory and analgesic activity, evident within 2 weeks, was sustained throughout the 12-week study. (nih.gov)
  • Hemicrania was mentioned in 1881 in The Therapeutic Gazette Vol. 2, by G.S.Davis, and the incident has been cited in King's American Dispensatory (1898 and later editions) in the description of the strong analgesic Jamaican Dogwood, a relatively low dose of which reportedly produced convulsions and prolonged respiratory depression over six hours in an elderly woman with this condition. (wikipedia.org)
  • potent
  • The researchers were able to achieve similar heart-stopping results in rat cardiac cells, whereas aspirin, another potent COX-2 inhibitor, had no effect, confirming that another mechanism is at work. (newsinferno.com)
  • inflammatory
  • COX-2 inhibitors have been found to be effective in suppressing inflammatory neurodegenerative pathways in mental illness, with beneficial results in trials for major depressive disorder as well as schizophrenia . (wikipedia.org)
  • COX-2 plays a major role in prostaglandin biosynthesis in inflammatory cells and in the central nervous system. (wikipedia.org)
  • however, the upregulation of pro-inflammatory COX-2 and increased production of COX-2 derived metabolites have been implicated in diabetic nephropathy. (innovations-report.com)
  • clinical trials
  • After several COX-2 inhibiting drugs were approved for marketing, data from clinical trials revealed that COX-2 inhibitors caused a significant increase in heart attacks and strokes, with some drugs in the class having worse risks than others. (wikipedia.org)
  • novel
  • In 1991, during the investigation of the expression of early-response genes in fibroblasts transformed with Rous sarcoma virus, a novel mRNA transcript that was similar, but not identical, to the seminal COX enzyme was identified. (wikipedia.org)
  • Another group discovered a novel cDNA species encoding a protein with similar structure to COX-1 while studying phorbol-ester-induced genes in Swiss 3T3 cells. (wikipedia.org)
  • The same laboratory showed that this gene truly expressed a novel COX enzyme. (wikipedia.org)
  • drugs
  • They also stress it is too early to speculate on human effects, although their results suggest Drosophilaâ€"one of the most valuable of organisms in biological research and has been used as a model research organism for almost a centuryâ€"are a valuable tool to investigate other COX-2 drugs. (newsinferno.com)
  • On September 2, 2009, the United States Department of Justice fined Pfizer $2.3 billion after one of its subsidiaries, Pharmacia & UpJohn Company, pleaded guilty to marketing four drugs including Bextra "with the intent to defraud or mislead. (wikipedia.org)
  • After widespread adoption of the COX-2 inhibitors, it was discovered that most of the drugs in this class increase the risk of cardiovascular events by 40% on average. (wikipedia.org)
  • effects
  • See 'COX-2 selective inhibitors: Adverse cardiovascular effects' . (uptodate.com)
  • To study the effects of COX-2 on PanIN progression, Dr. Eibl and colleagues focused on the KrasG12D mouse, an animal model that mimics the early stages of pancreatic cancer. (innovations-report.com)
  • In the future, Dr. Eibl and others plan to study the long-term effects of nimesulide and additional COX-2 inhibitors on the onset and progression of pancreatic cancer. (innovations-report.com)
  • Inc. (Novartis) to remove (recall) all lumiracoxib from local drug stores in 2 weeks due to the harmful effects of the drug (potential serious liver-related side effects, hepatotoxicity or malfunction of the lungs). (wikipedia.org)
  • Tramadol is structurally closer to venlafaxine than to codeine and delivers analgesia by not only delivering "opioid-like" effects (through mild agonism of the mu receptor) but also by acting as a weak but fast-acting serotonin releasing agent and norepinephrine reuptake inhibitor. (wikipedia.org)
  • disorders
  • Mark Thompson, "Hemicrania Continua" "The International Classification of Headache Disorders 2nd Edition (ICHD-2)" (PDF). (wikipedia.org)
  • kidney
  • A new study tests the hypothesis that altered kidney regulation of COX-2 occurs at a very early stage in the progression of kidney disease. (innovations-report.com)
  • increased COX-2 protein expression was observed in the kidney cortex and microvessels of the Obese Zucker rats at 10-12 and 20-21 weeks of age. (innovations-report.com)
  • treatment
  • 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfon-amide), the only FDA approved COX-2 inhibitor, has been used in the treatment of OA [ 13 , 14 ]. (hindawi.com)
  • Often blood transfusions are not recommended unless the hemoglobin is less than 70 or 80 g/L. Treatment with proton pump inhibitors, octreotide, and antibiotics may be considered in certain cases. (wikipedia.org)
  • prevention
  • The study, published in the August 1 issue of Cancer Research, a journal of the American Association for Cancer Research, suggests a potential role for COX-2 inhibitors in pancreatic cancer prevention among high-risk patients. (innovations-report.com)
  • pain
  • It treats pain mainly by blocking COX-2 mostly in the central nervous system, but not much in the rest of the body. (wikipedia.org)
  • analogue
  • Reaction of the imine with TosMIC in the presence of potassium carbonate leads to what may be viewed as 2+3 cycloaddition of the nitrogen analogue of a ketene to form the imidazole ring. (wikipedia.org)
  • leads
  • Encouraged by the "concept testing" experiments with selective inhibitors, and armed with several solid leads and clear idea of the nature of the binding site, development of this field was rapid. (wikipedia.org)