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MF498 [N-{[4-(5,9-Diethoxy-6-oxo-6,8-dihydro-7H-pyrrolo[3,4-g]quinolin-7-yl)-3-methylbenzyl]sulfonyl}-2-(2-methoxyphenyl)acetamide], a selective E prostanoid receptor 4 antagonist, relieves joint inflammation and pain in rodent models of rheumatoid and osteoarthritis.
Clark P, Rowland SE, Denis D, Mathieu MC, Stocco R, Poirier H, Burch J, Han Y, Audoly L, Therien AG, Xu D. Clark P, et al. Among authors: mathieu mc. J Pharmacol Exp Ther. 2008 May;325(2):425-34. doi: 10.1124/jpet.107.134510. Epub 2008 Feb 20. J Pharmacol Exp Ther. 2008. PMID: 18287210
Structure-activity relationships and pharmacokinetic parameters of quinoline acylsulfonamides as potent and selective antagonists of the EP(4) receptor.
Burch JD, Belley M, Fortin R, Deschênes D, Girard M, Colucci J, Farand J, Therien AG, Mathieu MC, Denis D, Vigneault E, Lévesque JF, Gagné S, Wrona M, Xu D, Clark P, Rowland S, Han Y. Burch JD, et al. Among authors: mathieu mc. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2048-54. doi: 10.1016/j.bmcl.2008.01.103. Epub 2008 Jan 31. Bioorg Med Chem Lett. 2008. PMID: 18291643
The discovery of 4-{1-[({2,5-dimethyl-4-[4-(trifluoromethyl)benzyl]-3-thienyl}carbonyl)amino]cyclopropyl}benzoic acid (MK-2894), a potent and selective prostaglandin E2 subtype 4 receptor antagonist.
Blouin M, Han Y, Burch J, Farand J, Mellon C, Gaudreault M, Wrona M, Lévesque JF, Denis D, Mathieu MC, Stocco R, Vigneault E, Therien A, Clark P, Rowland S, Xu D, O'Neill G, Ducharme Y, Friesen R. Blouin M, et al. Among authors: mathieu mc. J Med Chem. 2010 Mar 11;53(5):2227-38. doi: 10.1021/jm901771h. J Med Chem. 2010. PMID: 20163116
Discovery of 4-[1-[([1-[4-(trifluoromethyl)benzyl]-1H-indol-7-yl]carbonyl)amino]cyclopropyl]benzoic acid (MF-766), a highly potent and selective EP4 antagonist for treating inflammatory pain.
Colucci J, Boyd M, Berthelette C, Chiasson JF, Wang Z, Ducharme Y, Friesen R, Wrona M, Levesque JF, Denis D, Mathieu MC, Stocco R, Therien AG, Clarke P, Rowland S, Xu D, Han Y. Colucci J, et al. Among authors: mathieu mc. Bioorg Med Chem Lett. 2010 Jun 15;20(12):3760-3. doi: 10.1016/j.bmcl.2010.04.065. Epub 2010 Apr 18. Bioorg Med Chem Lett. 2010. PMID: 20471829
Naphthalene/quinoline amides and sulfonylureas as potent and selective antagonists of the EP4 receptor.
Burch JD, Farand J, Colucci J, Sturino C, Ducharme Y, Friesen RW, Lévesque JF, Gagné S, Wrona M, Therien AG, Mathieu MC, Denis D, Vigneault E, Xu D, Clark P, Rowland S, Han Y. Burch JD, et al. Among authors: mathieu mc. Bioorg Med Chem Lett. 2011 Feb 1;21(3):1041-6. doi: 10.1016/j.bmcl.2010.12.014. Epub 2010 Dec 8. Bioorg Med Chem Lett. 2011. PMID: 21215624
The C3a receptor antagonist SB 290157 has agonist activity.
Mathieu MC, Sawyer N, Greig GM, Hamel M, Kargman S, Ducharme Y, Lau CK, Friesen RW, O'Neill GP, Gervais FG, Therien AG. Mathieu MC, et al. Immunol Lett. 2005 Sep 15;100(2):139-45. doi: 10.1016/j.imlet.2005.03.003. Epub 2005 Mar 25. Immunol Lett. 2005. PMID: 16154494
170 results