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Page 1
Pharmacology of AM803, a novel selective five-lipoxygenase-activating protein (FLAP) inhibitor in rodent models of acute inflammation.
Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich PP, Darlington JV, Stock NS, Zunic J, King CD, Lee C, Baccei CS, Stearns B, Roppe J, Hutchinson JH, Prasit P, Evans JF. Lorrain DS, et al. Among authors: bain g. Eur J Pharmacol. 2010 Aug 25;640(1-3):211-8. doi: 10.1016/j.ejphar.2010.05.003. Epub 2010 May 21. Eur J Pharmacol. 2010. PMID: 20519143
Pharmacodynamics and pharmacokinetics of AM103, a novel inhibitor of 5-lipoxygenase-activating protein (FLAP).
Bain G, King CD, Rewolinski M, Schaab K, Santini AM, Shapiro D, Moran M, van de Wetering de Rooij S, Roffel AF, Schuilenga-Hut P, Milne GL, Lorrain DS, Li Y, Arruda JM, Hutchinson JH, Prasit P, Evans JF. Bain G, et al. Clin Pharmacol Ther. 2010 Apr;87(4):437-44. doi: 10.1038/clpt.2009.301. Epub 2010 Feb 24. Clin Pharmacol Ther. 2010. PMID: 20182424 Clinical Trial.
Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist.
Swaney JS, Chapman C, Correa LD, Stebbins KJ, Broadhead AR, Bain G, Santini AM, Darlington J, King CD, Baccei CS, Lee C, Parr TA, Roppe JR, Seiders TJ, Ziff J, Prasit P, Hutchinson JH, Evans JF, Lorrain DS. Swaney JS, et al. Among authors: bain g. J Pharmacol Exp Ther. 2011 Mar;336(3):693-700. doi: 10.1124/jpet.110.175901. Epub 2010 Dec 15. J Pharmacol Exp Ther. 2011. PMID: 21159750
5-lipoxygenase-activating protein inhibitors: development of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103).
Hutchinson JH, Li Y, Arruda JM, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King CD, Lee C, Lorrain D, Prodanovich P, Rong H, Santini A, Stock N, Prasit P, Evans JF. Hutchinson JH, et al. Among authors: bain g. J Med Chem. 2009 Oct 8;52(19):5803-15. doi: 10.1021/jm900945d. J Med Chem. 2009. PMID: 19739647
Pharmacological characterization of 3-[3-tert-butylsulfanyl-1-[4-(6-methoxy-pyridin-3-yl)-benzyl]-5-(pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM103), a novel selective 5-lipoxygenase-activating protein inhibitor that reduces acute and chronic inflammation.
Lorrain DS, Bain G, Correa LD, Chapman C, Broadhead AR, Santini AM, Prodanovich P, Darlington JV, Hutchinson JH, King C, Lee C, Baccei C, Li Y, Arruda JM, Evans JF. Lorrain DS, et al. Among authors: bain g. J Pharmacol Exp Ther. 2009 Dec;331(3):1042-50. doi: 10.1124/jpet.109.158089. Epub 2009 Sep 11. J Pharmacol Exp Ther. 2009. PMID: 19749079
5-Lipoxygenase-activating protein inhibitors. Part 2: 3-{5-((S)-1-Acetyl-2,3-dihydro-1H-indol-2-ylmethoxy)-3-tert-butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-1H-indol-2-yl}-2,2-dimethyl-propionic acid (AM679)--a potent FLAP inhibitor.
Stock N, Baccei C, Bain G, Broadhead A, Chapman C, Darlington J, King C, Lee C, Li Y, Lorrain DS, Prodanovich P, Rong H, Santini A, Zunic J, Evans JF, Hutchinson JH, Prasit P. Stock N, et al. Among authors: bain g. Bioorg Med Chem Lett. 2010 Jan 1;20(1):213-7. doi: 10.1016/j.bmcl.2009.10.131. Epub 2009 Oct 31. Bioorg Med Chem Lett. 2010. PMID: 19914828
Pharmacological blockade of the DP2 receptor inhibits cigarette smoke-induced inflammation, mucus cell metaplasia, and epithelial hyperplasia in the mouse lung.
Stebbins KJ, Broadhead AR, Baccei CS, Scott JM, Truong YP, Coate H, Stock NS, Santini AM, Fagan P, Prodanovich P, Bain G, Stearns BA, King CD, Hutchinson JH, Prasit P, Evans JF, Lorrain DS. Stebbins KJ, et al. Among authors: bain g. J Pharmacol Exp Ther. 2010 Mar;332(3):764-75. doi: 10.1124/jpet.109.161919. Epub 2009 Dec 8. J Pharmacol Exp Ther. 2010. PMID: 19996299
5-Lipoxygenase-activating protein inhibitors. Part 3: 3-{3-tert-Butylsulfanyl-1-[4-(5-methoxy-pyrimidin-2-yl)-benzyl]-5-(5-methyl-pyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethyl-propionic acid (AM643)-A potent FLAP inhibitor suitable for topical administration.
Stock N, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Schaab K, Evans JF, Hutchinson JH, Prasit P. Stock N, et al. Among authors: bain g. Bioorg Med Chem Lett. 2010 Aug 1;20(15):4598-601. doi: 10.1016/j.bmcl.2010.06.011. Epub 2010 Jun 8. Bioorg Med Chem Lett. 2010. PMID: 20566292
Pharmacology of AM211, a potent and selective prostaglandin D2 receptor type 2 antagonist that is active in animal models of allergic inflammation.
Bain G, Lorrain DS, Stebbins KJ, Broadhead AR, Santini AM, Prodanovich P, Darlington J, King CD, Lee C, Baccei C, Stearns B, Troung Y, Hutchinson JH, Prasit P, Evans JF. Bain G, et al. J Pharmacol Exp Ther. 2011 Jul;338(1):290-301. doi: 10.1124/jpet.111.180430. Epub 2011 Apr 12. J Pharmacol Exp Ther. 2011. PMID: 21487069
5-Lipoxygenase-activating protein (FLAP) inhibitors. Part 4: development of 3-[3-tert-butylsulfanyl-1-[4-(6-ethoxypyridin-3-yl)benzyl]-5-(5-methylpyridin-2-ylmethoxy)-1H-indol-2-yl]-2,2-dimethylpropionic acid (AM803), a potent, oral, once daily FLAP inhibitor.
Stock NS, Bain G, Zunic J, Li Y, Ziff J, Roppe J, Santini A, Darlington J, Prodanovich P, King CD, Baccei C, Lee C, Rong H, Chapman C, Broadhead A, Lorrain D, Correa L, Hutchinson JH, Evans JF, Prasit P. Stock NS, et al. Among authors: bain g. J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7. J Med Chem. 2011. PMID: 22059882
368 results