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Items: 20

1.

Discovery of potent and selective PPARα/δ dual antagonists and initial biological studies.

Jacintho JD, Baccei CS, Bravo Y, Broadhead A, Chen A, Correa L, Fischer K, Laffitte B, Lee C, Lorrain DS, Messmer D, Prasit P, Stebbins KJ, Stock NS.

Bioorg Med Chem Lett. 2019 Feb 1;29(3):503-508. doi: 10.1016/j.bmcl.2018.12.045. Epub 2018 Dec 21.

PMID:
30594433
2.

In vitro and in vivo pharmacology of NXT629, a novel and selective PPARα antagonist.

Stebbins KJ, Broadhead AR, Cabrera G, Correa LD, Messmer D, Bundey R, Baccei C, Bravo Y, Chen A, Stock NS, Prasit P, Lorrain DS.

Eur J Pharmacol. 2017 Aug 15;809:130-140. doi: 10.1016/j.ejphar.2017.05.008. Epub 2017 May 5.

PMID:
28483457
3.

Stomatal acclimation to vapour pressure deficit doubles transpiration of small tree seedlings with warming.

Marchin RM, Broadhead AA, Bostic LE, Dunn RR, Hoffmann WA.

Plant Cell Environ. 2016 Oct;39(10):2221-34. doi: 10.1111/pce.12790. Epub 2016 Aug 12.

4.

Identification of the first potent, selective and bioavailable PPARα antagonist.

Bravo Y, Baccei CS, Broadhead A, Bundey R, Chen A, Clark R, Correa L, Jacintho JD, Lorrain DS, Messmer D, Stebbins K, Prasit P, Stock N.

Bioorg Med Chem Lett. 2014 May 15;24(10):2267-72. doi: 10.1016/j.bmcl.2014.03.090. Epub 2014 Apr 4.

PMID:
24745969
5.

Captured streams and springs in combined sewers: a review of the evidence, consequences and opportunities.

Broadhead AT, Horn R, Lerner DN.

Water Res. 2013 Sep 1;47(13):4752-66. doi: 10.1016/j.watres.2013.05.020. Epub 2013 May 24. Review.

PMID:
23810838
6.

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.

J Med Chem. 2011 Dec 8;54(23):8013-29. doi: 10.1021/jm2008369. Epub 2011 Nov 7.

PMID:
22059882
7.

DP2 (CRTh2) antagonism reduces ocular inflammation induced by allergen challenge and respiratory syncytial virus.

Stebbins KJ, Broadhead AR, Musiyenko A, Barik S, Scott JM, Truong YP, Stearns BA, Hutchinson JH, Prasit P, Evans JF, Lorrain DS.

Int Arch Allergy Immunol. 2012;157(3):259-68. doi: 10.1159/000328769. Epub 2011 Oct 28.

PMID:
22042170
8.

Discovery and optimization of a biphenylacetic acid series of prostaglandin D2 receptor DP2 antagonists with efficacy in a murine model of allergic rhinitis.

Scott JM, Baccei C, Bain G, Broadhead A, Evans JF, Fagan P, Hutchinson JH, King C, Lorrain DS, Lee C, Prasit P, Prodanovich P, Santini A, Stearns BA.

Bioorg Med Chem Lett. 2011 Nov 1;21(21):6608-12. doi: 10.1016/j.bmcl.2011.01.024. Epub 2011 Jan 11.

PMID:
21958540
9.

The antinociceptive effect of the asthma drug ibudilast in rat models of peripheral and central neuropathic pain.

Hama AT, Broadhead A, Lorrain DS, Sagen J.

J Neurotrauma. 2012 Feb 10;29(3):600-10. doi: 10.1089/neu.2011.1863. Epub 2011 Oct 19.

PMID:
21806469
10.

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.

J Pharmacol Exp Ther. 2011 Jul;338(1):290-301. doi: 10.1124/jpet.111.180430. Epub 2011 Apr 12.

PMID:
21487069
11.

Sodium [2'-[(cyclopropanecarbonyl-ethyl-amino)-methyl]-4'-(6-ethoxy-pyridin-3-yl)-6-methoxy-biphenyl-3-yl]-acetate (AM432): a potent, selective prostaglandin D2 receptor antagonist.

Stock N, Volkots D, Stebbins K, Broadhead A, Stearns B, Roppe J, Parr T, Baccei C, Bain G, Chapman C, Correa L, Darlington J, King C, Lee C, Lorrain DS, Prodanovich P, Santini A, Evans JF, Hutchinson JH, Prasit P.

Bioorg Med Chem Lett. 2011 Feb 1;21(3):1036-40. doi: 10.1016/j.bmcl.2010.12.016. Epub 2010 Dec 9.

PMID:
21211969
12.

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.

J Pharmacol Exp Ther. 2011 Mar;336(3):693-700. doi: 10.1124/jpet.110.175901. Epub 2010 Dec 15.

PMID:
21159750
13.

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.

Eur J Pharmacol. 2010 Aug 25;640(1-3):211-8. doi: 10.1016/j.ejphar.2010.05.003. Epub 2010 May 21.

PMID:
20519143
14.

Therapeutic efficacy of AM156, a novel prostanoid DP2 receptor antagonist, in murine models of allergic rhinitis and house dust mite-induced pulmonary inflammation.

Stebbins KJ, Broadhead AR, Correa LD, Scott JM, Truong YP, Stearns BA, Hutchinson JH, Prasit P, Evans JF, Lorrain DS.

Eur J Pharmacol. 2010 Jul 25;638(1-3):142-9. doi: 10.1016/j.ejphar.2010.04.031. Epub 2010 May 4.

PMID:
20447387
15.

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.

J Pharmacol Exp Ther. 2010 Mar;332(3):764-75. doi: 10.1124/jpet.109.161919. Epub 2009 Dec 8.

PMID:
19996299
16.

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.

Bioorg Med Chem Lett. 2010 Jan 1;20(1):213-7. doi: 10.1016/j.bmcl.2009.10.131. Epub 2009 Oct 31.

PMID:
19914828
17.

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.

J Pharmacol Exp Ther. 2009 Dec;331(3):1042-50. doi: 10.1124/jpet.109.158089. Epub 2009 Sep 11.

PMID:
19749079
18.

Novel tricyclic antagonists of the prostaglandin D2 receptor DP2 with efficacy in a murine model of allergic rhinitis.

Stearns BA, Baccei C, Bain G, Broadhead A, Clark RC, Coate H, Evans JF, Fagan P, Hutchinson JH, King C, Lee C, Lorrain DS, Prasit P, Prodanovich P, Santini A, Scott JM, Stock NS, Truong YP.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4647-51. doi: 10.1016/j.bmcl.2009.06.085. Epub 2009 Jun 25.

PMID:
19608418
19.
20.

Geographic and breed distribution of an Msp I PCR-RFLP in the bovine growth hormone (bGH) gene.

Lagziel A, DeNise S, Hanotte O, Dhara S, Glazko V, Broadhead A, Davoli R, Russo V, Soller M.

Anim Genet. 2000 Jun;31(3):210-3.

PMID:
10895313

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