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Items: 46

1.

Discovery of GSK3527497: A Candidate for the Inhibition of Transient Receptor Potential Vanilloid-4 (TRPV4).

Brooks CA, Barton LS, Behm DJ, Brnardic EJ, Costell MH, Holt DA, Jolivette LJ, Matthews JM, McAtee JJ, McCleland BW, Patterson JR, Pero JE, Rivero RA, Roethke TJ, Sanchez RM, Shenje R, Terrell LR, Lawhorn BG.

J Med Chem. 2019 Oct 24;62(20):9270-9280. doi: 10.1021/acs.jmedchem.9b01247. Epub 2019 Oct 9.

PMID:
31532662
2.

Discovery of GSK2798745: A Clinical Candidate for Inhibition of Transient Receptor Potential Vanilloid 4 (TRPV4).

Brooks CA, Barton LS, Behm DJ, Eidam HS, Fox RM, Hammond M, Hoang TH, Holt DA, Hilfiker MA, Lawhorn BG, Patterson JR, Stoy P, Roethke TJ, Ye G, Zhao S, Thorneloe KS, Goodman KB, Cheung M.

ACS Med Chem Lett. 2019 Jul 15;10(8):1228-1233. doi: 10.1021/acsmedchemlett.9b00274. eCollection 2019 Aug 8.

PMID:
31413810
3.

Design and Optimization of Sulfone Pyrrolidine Sulfonamide Antagonists of Transient Receptor Potential Vanilloid-4 with in Vivo Activity in a Pulmonary Edema Model.

Pero JE, Matthews JM, Behm DJ, Brnardic EJ, Brooks C, Budzik BW, Costell MH, Donatelli CA, Eisennagel SH, Erhard K, Fischer MC, Holt DA, Jolivette LJ, Li H, Li P, McAtee JJ, McCleland BW, Pendrak I, Posobiec LM, Rivera KLK, Rivero RA, Roethke TJ, Sender MR, Shu A, Terrell LR, Vaidya K, Xu X, Lawhorn BG.

J Med Chem. 2018 Dec 27;61(24):11209-11220. doi: 10.1021/acs.jmedchem.8b01344. Epub 2018 Dec 12.

PMID:
30500190
4.

Discovery of Pyrrolidine Sulfonamides as Selective and Orally Bioavailable Antagonists of Transient Receptor Potential Vanilloid-4 (TRPV4).

Brnardic EJ, Ye G, Brooks C, Donatelli C, Barton L, McAtee J, Sanchez RM, Shu A, Erhard K, Terrell L, Graczyk-Millbrandt G, He Y, Costell MH, Behm DJ, Roethke T, Stoy P, Holt DA, Lawhorn BG.

J Med Chem. 2018 Nov 8;61(21):9738-9755. doi: 10.1021/acs.jmedchem.8b01317. Epub 2018 Oct 18.

PMID:
30335378
5.

Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4.

Cheung M, Bao W, Behm DJ, Brooks CA, Bury MJ, Dowdell SE, Eidam HS, Fox RM, Goodman KB, Holt DA, Lee D, Roethke TJ, Willette RN, Xu X, Ye G, Thorneloe KS.

ACS Med Chem Lett. 2017 Mar 20;8(5):549-554. doi: 10.1021/acsmedchemlett.7b00094. eCollection 2017 May 11.

6.

Toward improved myocardial maturity in an organ-on-chip platform with immature cardiac myocytes.

Sheehy SP, Grosberg A, Qin P, Behm DJ, Ferrier JP, Eagleson MA, Nesmith AP, Krull D, Falls JG, Campbell PH, McCain ML, Willette RN, Hu E, Parker KK.

Exp Biol Med (Maywood). 2017 Nov;242(17):1643-1656. doi: 10.1177/1535370217701006. Epub 2017 Mar 26.

7.

Discovery of 1-(1,3,5-triazin-2-yl)piperidine-4-carboxamides as inhibitors of soluble epoxide hydrolase.

Thalji RK, McAtee JJ, Belyanskaya S, Brandt M, Brown GD, Costell MH, Ding Y, Dodson JW, Eisennagel SH, Fries RE, Gross JW, Harpel MR, Holt DA, Israel DI, Jolivette LJ, Krosky D, Li H, Lu Q, Mandichak T, Roethke T, Schnackenberg CG, Schwartz B, Shewchuk LM, Xie W, Behm DJ, Douglas SA, Shaw AL, Marino JP Jr.

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3584-8. doi: 10.1016/j.bmcl.2013.04.019. Epub 2013 Apr 16.

PMID:
23664879
8.

Effects of Urotensin II Receptor Antagonist, GSK1440115, in Asthma.

Portnoy A, Kumar S, Behm DJ, Mahar KM, Noble RB, Throup JP, Russ SF.

Front Pharmacol. 2013 Apr 29;4:54. doi: 10.3389/fphar.2013.00054. eCollection 2013.

9.

In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor.

Podolin PL, Bolognese BJ, Foley JF, Long E 3rd, Peck B, Umbrecht S, Zhang X, Zhu P, Schwartz B, Xie W, Quinn C, Qi H, Sweitzer S, Chen S, Galop M, Ding Y, Belyanskaya SL, Israel DI, Morgan BA, Behm DJ, Marino JP Jr, Kurali E, Barnette MS, Mayer RJ, Booth-Genthe CL, Callahan JF.

Prostaglandins Other Lipid Mediat. 2013 Jul-Aug;104-105:25-31. doi: 10.1016/j.prostaglandins.2013.02.001. Epub 2013 Feb 19.

PMID:
23434473
10.

Urotensin II receptor antagonism confers vasoprotective effects in diabetes associated atherosclerosis: studies in humans and in a mouse model of diabetes.

Watson AM, Olukman M, Koulis C, Tu Y, Samijono D, Yuen D, Lee C, Behm DJ, Cooper ME, Jandeleit-Dahm KA, Calkin AC, Allen TJ.

Diabetologia. 2013 May;56(5):1155-65. doi: 10.1007/s00125-013-2837-9. Epub 2013 Jan 24.

PMID:
23344731
11.

Soluble epoxide hydrolase inhibition does not prevent cardiac remodeling and dysfunction after aortic constriction in rats and mice.

Morgan LA, Olzinski AR, Upson JJ, Zhao S, Wang T, Eisennagel SH, Hoang B, Tunstead JR, Marino JP Jr, Willette RN, Jucker BM, Behm DJ.

J Cardiovasc Pharmacol. 2013 Apr;61(4):291-301. doi: 10.1097/FJC.0b013e31827fe59c.

PMID:
23232840
12.

Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress.

Costell MH, Ancellin N, Bernard RE, Zhao S, Upson JJ, Morgan LA, Maniscalco K, Olzinski AR, Ballard VL, Herry K, Grondin P, Dodic N, Mirguet O, Bouillot A, Gellibert F, Coatney RW, Lepore JJ, Jucker BM, Jolivette LJ, Willette RN, Schnackenberg CG, Behm DJ.

Front Pharmacol. 2012 Jul 5;3:128. doi: 10.3389/fphar.2012.00128. eCollection 2012.

13.

Genetic and pharmacological manipulation of urotensin II ameliorate the metabolic and atherosclerosis sequalae in mice.

You Z, Genest J Jr, Barrette PO, Hafiane A, Behm DJ, D'Orleans-Juste P, Schwertani AG.

Arterioscler Thromb Vasc Biol. 2012 Aug;32(8):1809-16. doi: 10.1161/ATVBAHA.112.252973. Epub 2012 Jun 21.

PMID:
22723440
14.

Soluble epoxide hydrolase inhibition exerts beneficial anti-remodeling actions post-myocardial infarction.

Kompa AR, Wang BH, Xu G, Zhang Y, Ho PY, Eisennagel S, Thalji RK, Marino JP Jr, Kelly DJ, Behm DJ, Krum H.

Int J Cardiol. 2013 Jul 15;167(1):210-9. doi: 10.1016/j.ijcard.2011.12.062. Epub 2012 Jan 10.

PMID:
22236509
15.

Urotensin II differentially regulates macrophage and hepatic cholesterol homeostasis.

Kiss RS, You Z, Genest J Jr, Behm DJ, Giaid A.

Peptides. 2011 May;32(5):956-63. doi: 10.1016/j.peptides.2011.02.016. Epub 2011 Mar 2.

PMID:
21376094
16.

GSK1562590, a slowly dissociating urotensin-II receptor antagonist, exhibits prolonged pharmacodynamic activity ex vivo.

Behm DJ, Aiyar NV, Olzinski AR, McAtee JJ, Hilfiker MA, Dodson JW, Dowdell SE, Wang GZ, Goodman KB, Sehon CA, Harpel MR, Willette RN, Neeb MJ, Leach CA, Douglas SA.

Br J Pharmacol. 2010 Sep;161(1):207-28. doi: 10.1111/j.1476-5381.2010.00889.x.

17.

Chronic inhibition of hypoxia-inducible factor prolyl 4-hydroxylase improves ventricular performance, remodeling, and vascularity after myocardial infarction in the rat.

Bao W, Qin P, Needle S, Erickson-Miller CL, Duffy KJ, Ariazi JL, Zhao S, Olzinski AR, Behm DJ, Pipes GC, Jucker BM, Hu E, Lepore JJ, Willette RN.

J Cardiovasc Pharmacol. 2010 Aug;56(2):147-55. doi: 10.1097/FJC.0b013e3181e2bfef.

PMID:
20714241
18.

Chronic urotensin II receptor antagonist treatment does not alter hypertrophy or fibrosis in a rat model of pressure-overload hypertrophy.

Kompa AR, Wang BH, Phrommintikul A, Ho PY, Kelly DJ, Behm DJ, Douglas SA, Krum H.

Peptides. 2010 Aug;31(8):1523-30. doi: 10.1016/j.peptides.2010.04.026. Epub 2010 May 7.

PMID:
20452383
19.

Differential effects of p38 mitogen-activated protein kinase and cyclooxygenase 2 inhibitors in a model of cardiovascular disease.

Willette RN, Eybye ME, Olzinski AR, Behm DJ, Aiyar N, Maniscalco K, Bentley RG, Coatney RW, Zhao S, Westfall TD, Doe CP.

J Pharmacol Exp Ther. 2009 Sep;330(3):964-70. doi: 10.1124/jpet.109.154443. Epub 2009 Jun 25.

PMID:
19556450
20.

Targeted overexpression of the human urotensin receptor transgene in smooth muscle cells: effect of UT antagonism in ApoE knockout mice fed with Western diet.

Papadopoulos P, Bousette N, Al-Ramli W, You Z, Behm DJ, Ohlstein EH, Harrison SM, Douglas SA, Giaid A.

Atherosclerosis. 2009 Jun;204(2):395-404. doi: 10.1016/j.atherosclerosis.2008.10.044. Epub 2008 Nov 21.

PMID:
19111831
21.

Potent, selective and orally bioavailable dihydropyrimidine inhibitors of Rho kinase (ROCK1) as potential therapeutic agents for cardiovascular diseases.

Sehon CA, Wang GZ, Viet AQ, Goodman KB, Dowdell SE, Elkins PA, Semus SF, Evans C, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D.

J Med Chem. 2008 Nov 13;51(21):6631-4. doi: 10.1021/jm8005096. Epub 2008 Oct 9.

PMID:
18842034
22.

Epoxyeicosatrienoic acids function as selective, endogenous antagonists of native thromboxane receptors: identification of a novel mechanism of vasodilation.

Behm DJ, Ogbonna A, Wu C, Burns-Kurtis CL, Douglas SA.

J Pharmacol Exp Ther. 2009 Jan;328(1):231-9. doi: 10.1124/jpet.108.145102. Epub 2008 Oct 3.

PMID:
18836067
23.

Aminomethylpiperazines as selective urotensin antagonists.

Hilfiker MA, Zhang D, Dowdell SE, Goodman KB, McAtee JJ, Dodson JW, Viet AQ, Wang GZ, Sehon CA, Behm DJ, Wu Z, Carballo LH, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4470-3. doi: 10.1016/j.bmcl.2008.07.067. Epub 2008 Jul 20.

PMID:
18674898
24.

Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues.

Behm DJ, McAtee JJ, Dodson JW, Neeb MJ, Fries HE, Evans CA, Hernandez RR, Hoffman KD, Harrison SM, Lai JM, Wu C, Aiyar NV, Ohlstein EH, Douglas SA.

Br J Pharmacol. 2008 Oct;155(3):374-86. doi: 10.1038/bjp.2008.266. Epub 2008 Jun 30.

25.

Potent and selective small-molecule human urotensin-II antagonists with improved pharmacokinetic profiles.

McAtee JJ, Dodson JW, Dowdell SE, Erhard K, Girard GR, Goodman KB, Hilfiker MA, Jin J, Sehon CA, Sha D, Shi D, Wang F, Wang GZ, Wang N, Wang Y, Viet AQ, Yuan CC, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jul 1;18(13):3716-9. doi: 10.1016/j.bmcl.2008.05.058. Epub 2008 May 20.

PMID:
18524591
26.

Development of potent and selective small-molecule human Urotensin-II antagonists.

McAtee JJ, Dodson JW, Dowdell SE, Girard GR, Goodman KB, Hilfiker MA, Sehon CA, Sha D, Wang GZ, Wang N, Viet AQ, Zhang D, Aiyar NV, Behm DJ, Carballo LH, Evans CA, Fries HE, Nagilla R, Roethke TJ, Xu X, Yuan CC, Douglas SA, Neeb MJ.

Bioorg Med Chem Lett. 2008 Jun 15;18(12):3500-3. doi: 10.1016/j.bmcl.2008.05.027. Epub 2008 May 10.

PMID:
18502123
27.

Systemic activation of the transient receptor potential vanilloid subtype 4 channel causes endothelial failure and circulatory collapse: Part 2.

Willette RN, Bao W, Nerurkar S, Yue TL, Doe CP, Stankus G, Turner GH, Ju H, Thomas H, Fishman CE, Sulpizio A, Behm DJ, Hoffman S, Lin Z, Lozinskaya I, Casillas LN, Lin M, Trout RE, Votta BJ, Thorneloe K, Lashinger ES, Figueroa DJ, Marquis R, Xu X.

J Pharmacol Exp Ther. 2008 Aug;326(2):443-52. doi: 10.1124/jpet.107.134551. Epub 2008 May 22. Erratum in: J Pharmacol Exp Ther. 2011 Jul;338(1):408-9.

PMID:
18499744
28.

2-Aminomethyl piperidines as novel urotensin-II receptor antagonists.

Jin J, Wang Y, Wang F, Shi D, Erhard KF, Wu Z, Guida BF, Lawrence SK, Behm DJ, Disa J, Vaidya KS, Evans C, McMillan LJ, Rivero RA, Neeb MJ, Douglas SA.

Bioorg Med Chem Lett. 2008 May 1;18(9):2860-4. doi: 10.1016/j.bmcl.2008.03.078. Epub 2008 Apr 8.

PMID:
18420409
29.

The novel endocannabinoid receptor GPR55 is activated by atypical cannabinoids but does not mediate their vasodilator effects.

Johns DG, Behm DJ, Walker DJ, Ao Z, Shapland EM, Daniels DA, Riddick M, Dowell S, Staton PC, Green P, Shabon U, Bao W, Aiyar N, Yue TL, Brown AJ, Morrison AD, Douglas SA.

Br J Pharmacol. 2007 Nov;152(5):825-31. Epub 2007 Aug 20.

30.

Effects of p38 MAPK Inhibitor on angiotensin II-dependent hypertension, organ damage, and superoxide anion production.

Bao W, Behm DJ, Nerurkar SS, Ao Z, Bentley R, Mirabile RC, Johns DG, Woods TN, Doe CP, Coatney RW, Ohlstein JF, Douglas SA, Willette RN, Yue TL.

J Cardiovasc Pharmacol. 2007 Jun;49(6):362-8.

PMID:
17577100
31.

Development of dihydropyridone indazole amides as selective Rho-kinase inhibitors.

Goodman KB, Cui H, Dowdell SE, Gaitanopoulos DE, Ivy RL, Sehon CA, Stavenger RA, Wang GZ, Viet AQ, Xu W, Ye G, Semus SF, Evans C, Fries HE, Jolivette LJ, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Jung DK, Wright LL, Smith GK, Behm DJ, Bentley R, Doe CP, Hu E, Lee D.

J Med Chem. 2007 Jan 11;50(1):6-9.

PMID:
17201405
32.

Discovery of aminofurazan-azabenzimidazoles as inhibitors of Rho-kinase with high kinase selectivity and antihypertensive activity.

Stavenger RA, Cui H, Dowdell SE, Franz RG, Gaitanopoulos DE, Goodman KB, Hilfiker MA, Ivy RL, Leber JD, Marino JP Jr, Oh HJ, Viet AQ, Xu W, Ye G, Zhang D, Zhao Y, Jolivette LJ, Head MS, Semus SF, Elkins PA, Kirkpatrick RB, Dul E, Khandekar SS, Yi T, Jung DK, Wright LL, Smith GK, Behm DJ, Doe CP, Bentley R, Chen ZX, Hu E, Lee D.

J Med Chem. 2007 Jan 11;50(1):2-5.

PMID:
17201404
33.

Novel Rho kinase inhibitors with anti-inflammatory and vasodilatory activities.

Doe C, Bentley R, Behm DJ, Lafferty R, Stavenger R, Jung D, Bamford M, Panchal T, Grygielko E, Wright LL, Smith GK, Chen Z, Webb C, Khandekar S, Yi T, Kirkpatrick R, Dul E, Jolivette L, Marino JP Jr, Willette R, Lee D, Hu E.

J Pharmacol Exp Ther. 2007 Jan;320(1):89-98. Epub 2006 Oct 3.

PMID:
17018693
34.

The peptidic urotensin-II receptor ligand GSK248451 possesses less intrinsic activity than the low-efficacy partial agonists SB-710411 and urantide in native mammalian tissues and recombinant cell systems.

Behm DJ, Stankus G, Doe CP, Willette RN, Sarau HM, Foley JJ, Schmidt DB, Nuthulaganti P, Fornwald JA, Ames RS, Lambert DG, Calo' G, Camarda V, Aiyar NV, Douglas SA.

Br J Pharmacol. 2006 May;148(2):173-90.

35.

Inhibitory effects of putative peptidic urotensin-II receptor antagonists on urotensin-II-induced contraction of cat isolated respiratory smooth muscle.

Behm DJ, Ao Z, Camarda V, Aiyar NV, Johns DG, Douglas SA.

Eur J Pharmacol. 2005 Jun 15;516(3):276-81.

PMID:
15975570
36.

Nonpeptidic urotensin-II receptor antagonists I: in vitro pharmacological characterization of SB-706375.

Douglas SA, Behm DJ, Aiyar NV, Naselsky D, Disa J, Brooks DP, Ohlstein EH, Gleason JG, Sarau HM, Foley JJ, Buckley PT, Schmidt DB, Wixted WE, Widdowson K, Riley G, Jin J, Gallagher TF, Schmidt SJ, Ridgers L, Christmann LT, Keenan RM, Knight SD, Dhanak D.

Br J Pharmacol. 2005 Jul;145(5):620-35.

37.

Hypertensive target organ damage is attenuated by a p38 MAPK inhibitor: role of systemic blood pressure and endothelial protection.

Olzinski AR, McCafferty TA, Zhao SQ, Behm DJ, Eybye ME, Maniscalco K, Bentley R, Frazier KS, Milliner CM, Mirabile RC, Coatney RW, Willette RN.

Cardiovasc Res. 2005 Apr 1;66(1):170-8. Epub 2005 Jan 28.

PMID:
15769460
38.

Cloning and pharmacological characterization of the cat urotensin-II receptor (UT).

Aiyar N, Johns DG, Ao Z, Disa J, Behm DJ, Foley JJ, Buckley PT, Sarau HM, van-der-Keyl HK, Elshourbagy NA, Douglas SA.

Biochem Pharmacol. 2005 Apr 1;69(7):1069-79.

PMID:
15763543
39.

Urantide mimics urotensin-II induced calcium release in cells expressing recombinant UT receptors.

Camarda V, Song W, Marzola E, Spagnol M, Guerrini R, Salvadori S, Regoli D, Thompson JP, Rowbotham DJ, Behm DJ, Douglas SA, Calo' G, Lambert DG.

Eur J Pharmacol. 2004 Sep 13;498(1-3):83-6.

PMID:
15363979
40.

Differential levels of "urotensin-II-like" activity determined by radio-receptor and radioimmuno-assays.

Aiyar N, Guida B, Ao Z, Disa J, Naselsky D, Behm DJ, Su JL, Kull FC Jr, Douglas SA.

Peptides. 2004 Aug;25(8):1339-47.

PMID:
15350702
41.

Differential agonistic and antagonistic effects of the urotensin-II ligand SB-710411 at rodent and primate UT receptors.

Behm DJ, Herold CL, Camarda V, Aiyar NV, Douglas SA.

Eur J Pharmacol. 2004 May 25;492(2-3):113-6.

PMID:
15178353
42.

Urotensin-II: a novel systemic hypertensive factor in the cat.

Behm DJ, Doe CP, Johns DG, Maniscalco K, Stankus GP, Wibberley A, Willette RN, Douglas SA.

Naunyn Schmiedebergs Arch Pharmacol. 2004 Mar;369(3):274-80. Epub 2004 Feb 19.

PMID:
14985938
43.

p38 MAPK inhibitors ameliorate target organ damage in hypertension: Part 1. p38 MAPK-dependent endothelial dysfunction and hypertension.

Ju H, Behm DJ, Nerurkar S, Eybye ME, Haimbach RE, Olzinski AR, Douglas SA, Willette RN.

J Pharmacol Exp Ther. 2003 Dec;307(3):932-8. Epub 2003 Oct 15.

PMID:
14561851
44.

Deletion of the UT receptor gene results in the selective loss of urotensin-II contractile activity in aortae isolated from UT receptor knockout mice.

Behm DJ, Harrison SM, Ao Z, Maniscalco K, Pickering SJ, Grau EV, Woods TN, Coatney RW, Doe CP, Willette RN, Johns DG, Douglas SA.

Br J Pharmacol. 2003 May;139(2):464-72.

45.

The neuromedin B receptor antagonist, BIM-23127, is a potent antagonist at human and rat urotensin-II receptors.

Herold CL, Behm DJ, Buckley PT, Foley JJ, Wixted WE, Sarau HM, Douglas SA.

Br J Pharmacol. 2003 May;139(2):203-7.

46.

Pharmacological characterization of SB-710411 (Cpa-c[D-Cys-Pal-D-Trp-Lys-Val-Cys]-Cpa-amide), a novel peptidic urotensin-II receptor antagonist.

Behm DJ, Herold CL, Ohlstein EH, Knight SD, Dhanak D, Douglas SA.

Br J Pharmacol. 2002 Oct;137(4):449-58.

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