Access the full text.
Sign up today, get DeepDyve free for 14 days.
J. Couzin (2004)
Halt of Celebrex Study Threatens Drug's Future, Other TrialsScience, 306
K. Brune, B. Hinz (2004)
Selective cyclooxygenase‐2 inhibitors: similarities and differencesScandinavian Journal of Rheumatology, 33
J. Couzin (2004)
Clinical trials. Halt of Celebrex study threatens drug’s future, other trialsScience, 306
E. Ott, N. Nussmeier, P. Duke, R. Feneck, R. Alston, M. Snabes, R. Hubbard, P. Hsu, L. Saidman, L. Saidman, D. Mangano (2003)
Efficacy and safety of the cyclooxygenase 2 inhibitors parecoxib and valdecoxib in patients undergoing coronary artery bypass surgery.The Journal of thoracic and cardiovascular surgery, 125 6
A. Smith (1984)
Clinical trialsMedical Journal of Australia, 140
X. Leval, F. Julemont, V. Benoit, M. Frederich, B. Pirotte, J. M. Dogne (2004)
First and second generations of COX-2 selective inhibitorsMinirev. Med. Chem., 4
C. Bombardier, L. Laine, A. Reicin, D. Shapiro, R. Burgos-Vargas, B. Davis, R. Day, M. Ferraz, C. Hawkey, M. Hochberg, T. Kvien, T. Schnitzer (2000)
Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. VIGOR Study Group.The New England journal of medicine, 343 21
J. R. Lisse, M. Perlman, G. Johansson, J. R. Shoemaker, J. Schechtman, C. S. Skalky, M. E. Dixon, A. B. Polis, A. J. Mollen, G. P. Geba (2003)
Gastrointestinal tolerability and effectiveness of rofecoxib versus naproxen in the treatment of osteoarthritis: a randomized, controlled trialAnn. Intern. Med., 139
F. Silverstein, G. Faich, J. Goldstein, L. Simon, T. Pincus, A. Whelton, R. Makuch, G. Eisen, N. Agrawal, W. Stenson, A. Burr, William Zhao, J. Kent, J. Lefkowith, K. Verburg, G. Geis (2000)
Gastrointestinal toxicity with celecoxib vs nonsteroidal anti-inflammatory drugs for osteoarthritis and rheumatoid arthritis: the CLASS study: A randomized controlled trial. Celecoxib Long-term Arthritis Safety Study.JAMA, 284 10
J. Mitchell, T. Warner (1999)
Cyclo‐oxygenase‐2: pharmacology, physiology, biochemistry and relevance to NSAID therapyBritish Journal of Pharmacology, 128
J. Vane, Y. Bakhle, R. Botting (1998)
Cyclooxygenases 1 and 2.Annual review of pharmacology and toxicology, 38
Stefan Lohmander, D. McKeith, Ola Svensson, Maria Malmenäs, Lena Bolin, A. Kalla, György Genti, Jacek Szechinski, Cesar Ramos-Remus (2004)
A randomised, placebo controlled, comparative trial of the gastrointestinal safety and efficacy of AZD3582 versus naproxen in osteoarthritisAnnals of the Rheumatic Diseases, 64
D. Solomon, S. Schneeweiss, R. Glynn, Yuka Kiyota, R. Levin, H. Mogun, J. Avorn (2004)
Relationship Between Selective Cyclooxygenase-2 Inhibitors and Acute Myocardial Infarction in Older AdultsCirculation: Journal of the American Heart Association, 109
M. James, C. Hawkey (2003)
Assessment of non-steroidal anti-inflammatory drug (NSAID) damage in the human gastrointestinal tract.British journal of clinical pharmacology, 56 2
J. Fries (1999)
Gastrointestinal toxicity of nonsteroidal antiinflammatory drugs.The New England journal of medicine, 341 18
(2002)
Nitric oxide donor addition renders cyclooxygenase-2 (COX-2) selective inhibitors anti-thrombotic in vivo, Gut 51 (Suppl
J. Lisse, M. Perlman, G. Johansson, James Shoemaker, J. Schechtman, C. Skalky, M. Dixon, A. Polis, Arthur Mollen, G. Geba (2003)
Gastrointestinal Tolerability and Effectiveness of Rofecoxib versus Naproxen in the Treatment of OsteoarthritisAnnals of Internal Medicine, 139
A. Reicin, D. Shapiro, R. Sperling, E. Barr, Q. Yu (2002)
Comparison of cardiovascular thrombotic events in patients with osteoarthritis treated with rofecoxib versus nonselective nonsteroidal anti-inflammatory drugs (ibuprofen, diclofenac, and nabumetone).The American journal of cardiology, 89 2
M. Muscará, W. McKnight, P. Soldato, J. Wallace (1998)
Effect of a nitric oxide-releasing naproxen derivative on hypertension and gastric damage induced by chronic nitric oxide inhibition in the rat.Life sciences, 62 15
J. Masferrer, Bs Zweifel, Pt Manning, Sd Hauser, Km Leahy, W. Smith, P. Isakson, K. Seibert (1994)
Selective inhibition of inducible cyclooxygenase 2 in vivo is antiinflammatory and nonulcerogenic.Proceedings of the National Academy of Sciences of the United States of America, 91
L. Laine, E. Maller, Chang Yu, H. Quan, T. Simon (2004)
Ulcer formation with low-dose enteric-coated aspirin and the effect of COX-2 selective inhibition: a double-blind trial.Gastroenterology, 127 2
S. Kwiecień, T. Brzozowski, Konturek PCh, Konturek Sj (2002)
The role of reactive oxygen species in action of nitric oxide-donors on stress-induced gastric mucosal lesions.Journal of physiology and pharmacology : an official journal of the Polish Physiological Society, 53 4 Pt 2
James Brown, A. Keates, Peter Hanson, B. Whittle (1993)
Nitric oxide generators and cGMP stimulate mucus secretion by rat gastric mucosal cells.The American journal of physiology, 265 3 Pt 1
James Brown, Peter Hanson, Brendan Whittle (1992)
Nitric oxide donors increase mucus gel thickness in rat stomach.European journal of pharmacology, 223 1
(2003)
Multicenter Study of Perioperative Ischemia (McSPI) Research Group; Ischemia Research and Education Foundation (IREF
D. R. Janero, E. Cochran, X. Fang, D. S. Garvey, L. G. Letts, P. Marek, J. Schroeder (2002)
Nitric oxide donor addition renders cyclooxygenase-2 (COX-2) selective inhibitors anti-thrombotic in vivoGut, 51
M. Tramèr, R. Moore, D. Reynolds, H. McQuay (2000)
Quantitative estimation of rare adverse events which follow a biological progression: a new model applied to chronic NSAID usePain, 85
G. Rossoni, B. Manfredi, P. Soldato, F. Berti (2004)
The Nitric Oxide-Releasing Naproxen Derivative Displays Cardioprotection in Perfused Rabbit Heart Submitted to Ischemia-ReperfusionJournal of Pharmacology and Experimental Therapeutics, 310
G. Walford, J. Loscalzo (2003)
Nitric oxide in vascular biologyJournal of Thrombosis and Haemostasis, 1
C. Hawkey, John Jones, Clare Atherton, Maeve Skelly, J. Bebb, Urban Fagerholm, Bror Jonzon, Pär Karlsson, I. Bjarnason (2003)
Gastrointestinal safety of AZD3582, a cyclooxygenase inhibiting nitric oxide donator: proof of concept study in humansGut, 52
R. Ranatunge, M. Augustyniak, U. Bandarage, R. Earl, J. Ellis, D. Garvey, D. Janero, L. Letts, Allison Martino, Madhavi Murty, S. Richardson, J. Schroeder, M. Shumway, S. Tam, A. Trocha, D. Young (2004)
Synthesis and selective cyclooxygenase-2 inhibitory activity of a series of novel, nitric oxide donor-containing pyrazoles.Journal of medicinal chemistry, 47 9
X. Leval, F. Julémont, V. Benoit, M. Frédérich, B. Pirotte, J. Dogné (2004)
First and second generations of COX-2 selective inhibitors.Mini reviews in medicinal chemistry, 4 6
R. Flower (2003)
The development of COX2 inhibitorsNature Reviews Drug Discovery, 2
C. Winter, E. Risley, G. Nuss (1962)
Carrageenin-Induced Edema in Hind Paw of the Rat as an Assay for Antiinflammatory DrugsProceedings of the Society for Experimental Biology and Medicine, 111
M. Muscará, F. Lovren, W. McKnight, M. Dicay, P. Soldato, C. Triggle, J. Wallace (2001)
Vasorelaxant effects of a nitric oxide‐releasing aspirin derivative in normotensive and hypertensive ratsBritish Journal of Pharmacology, 133
S. Fiorucci, L. Santucci, J. Wallace, M. Sardina, M. Romano, P. Soldato, A. Morelli (2003)
Interaction of a selective cyclooxygenase-2 inhibitor with aspirin and NO-releasing aspirin in the human gastric mucosaProceedings of the National Academy of Sciences of the United States of America, 100
D. Mukherjee, S. Nissen, E. Topol (2001)
Risk of cardiovascular events associated with selective COX-2 inhibitors.JAMA, 286 8
P. Kubes, M. Suzuki, D. Granger (1991)
Nitric oxide: an endogenous modulator of leukocyte adhesion.Proceedings of the National Academy of Sciences of the United States of America, 88 11
J. Wallace, K. Chapman, W. McKnight (1999)
Limited anti‐inflammatory efficacy of cyclo‐oxygenase‐2 inhibition in carrageenan‐airpouch inflammationBritish Journal of Pharmacology, 126
Non-steroidal anti-inflammatory drugs (NSAIDs) are widely used to treat inflammation and to provide pain relief but suffer from a major liability concerning their propensity to cause gastric damage. As nitric oxide (NO) is known to be gastro-protective we have synthesized a NO-donating prodrug of naproxen named NMI-1182. We evaluated two cyclo-oxygenase (COX)-inhibiting nitric oxide donors (CINODs), NMI-1182 and AZD3582, for their ability to be gastroprotective compared to naproxen and for their anti-inflammatory activity. NMI-1182 and AZD3582 were found to produce similar inhibition of COX activity to that produced by naproxen. Both NMI-1182 and AZD3582 produced significantly less gastric lesions after oral administration than naproxen. All three compounds effectively inhibited paw swelling in the rat carrageenan paw edema model. In the carrageenan air pouch model all three compounds significantly reduced PGE2 levels in the pouch exudate but only NMI-1182 and naproxen inhibited leukocyte influx. These data demonstrate that NMI-1182 has comparable anti-inflammatory activity to naproxen but with a much reduced likelihood to cause gastric damage.
Inflammopharmacology – Springer Journals
Published: Jan 1, 2006
Read and print from thousands of top scholarly journals.
Already have an account? Log in
Bookmark this article. You can see your Bookmarks on your DeepDyve Library.
To save an article, log in first, or sign up for a DeepDyve account if you don’t already have one.
Copy and paste the desired citation format or use the link below to download a file formatted for EndNote
Access the full text.
Sign up today, get DeepDyve free for 14 days.
All DeepDyve websites use cookies to improve your online experience. They were placed on your computer when you launched this website. You can change your cookie settings through your browser.