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Items: 1 to 50 of 133

1.

Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases.

Salmon M, Luttmann MA, Foley JJ, Buckley PT, Schmidt DB, Burman M, Webb EF, DeHaas CJ, Kotzer CJ, Barrett VJ, Slack RJ, Sarau HM, Palovich MR, Lainé DI, Hay DW, Rumsey WL.

J Pharmacol Exp Ther. 2013 May;345(2):260-70. doi: 10.1124/jpet.112.202051. Epub 2013 Feb 22.

PMID:
23435542
2.

Tyrosine urea muscarinic acetylcholine receptor antagonists: achiral quaternary ammonium groups.

Jin Q, Davis RS, Bullion AM, Jin J, Wang Y, Widdowson KL, Palovich MR, Foley JJ, Schmidt DB, Buckley PT, Webb EF, Salmon M, Belmonte KE, Sarau HM, Busch-Petersen J.

Bioorg Med Chem Lett. 2012 Dec 1;22(23):7087-91. doi: 10.1016/j.bmcl.2012.09.085. Epub 2012 Oct 2.

PMID:
23099092
3.

Design, synthesis and structure-activity relationship of N-substituted tropane muscarinic acetylcholine receptor antagonists.

Lainé DI, Yan H, Xie H, Davis RS, Dufour J, Widdowson KL, Palovich MR, Wan Z, Foley JJ, Schmidt DB, Hunsberger GE, Burman M, Bacon AM, Webb EF, Luttmann MA, Salmon M, Sarau HM, Umbrecht ST, Landis PS, Peck BJ, Busch-Petersen J.

Bioorg Med Chem Lett. 2012 May 1;22(9):3366-9. doi: 10.1016/j.bmcl.2012.02.015. Epub 2012 Feb 15.

PMID:
22460029
4.

Design, synthesis, and structure-activity relationship of tropane muscarinic acetylcholine receptor antagonists.

Lainé DI, Wan Z, Yan H, Zhu C, Xie H, Fu W, Busch-Petersen J, Neipp C, Davis R, Widdowson KL, Blaney FE, Foley J, Bacon AM, Webb EF, Luttmann MA, Burman M, Sarau HM, Salmon M, Palovich MR, Belmonte K.

J Med Chem. 2009 Aug 27;52(16):5241-52. doi: 10.1021/jm900736e.

PMID:
19630384
5.

Discovery of (3-endo)-3-(2-cyano-2,2-diphenylethyl)-8,8-dimethyl-8-azoniabicyclo[3.2.1]octane bromide as an efficacious inhaled muscarinic acetylcholine receptor antagonist for the treatment of COPD.

Wan Z, Laine DI, Yan H, Zhu C, Widdowson KL, Buckley PT, Burman M, Foley JJ, Sarau HM, Schmidt DB, Webb EF, Belmonte KE, Palovich M.

Bioorg Med Chem Lett. 2009 Aug 15;19(16):4560-2. doi: 10.1016/j.bmcl.2009.07.006. Epub 2009 Jul 8.

PMID:
19616944
6.

M3 muscarinic acetylcholine receptor antagonists: SAR and optimization of bi-aryl amines.

Budzik B, Wang Y, Shi D, Wang F, Xie H, Wan Z, Zhu C, Foley JJ, Nuthulaganti P, Kallal LA, Sarau HM, Morrow DM, Moore ML, Rivero RA, Palovich M, Salmon M, Belmonte KE, Laine DI, Jin J.

Bioorg Med Chem Lett. 2009 Mar 15;19(6):1686-90. doi: 10.1016/j.bmcl.2009.01.098. Epub 2009 Feb 4.

PMID:
19243945
7.

Camphor sulfonamide derivatives as novel, potent and selective CXCR3 antagonists.

Wang Y, Busch-Petersen J, Wang F, Kiesow TJ, Graybill TL, Jin J, Yang Z, Foley JJ, Hunsberger GE, Schmidt DB, Sarau HM, Capper-Spudich EA, Wu Z, Fisher LS, McQueney MS, Rivero RA, Widdowson KL.

Bioorg Med Chem Lett. 2009 Jan 1;19(1):114-8. doi: 10.1016/j.bmcl.2008.11.008. Epub 2008 Nov 6.

PMID:
19014886
8.

Muscarinic acetylcholine receptor antagonists: SAR and optimization of tyrosine ureas.

Jin J, Wang Y, Shi D, Wang F, Fu W, Davis RS, Jin Q, Foley JJ, Sarau HM, Morrow DM, Moore ML, Rivero RA, Palovich M, Salmon M, Belmonte KE, Busch-Petersen J.

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5481-6. doi: 10.1016/j.bmcl.2008.09.020. Epub 2008 Sep 10.

PMID:
18818072
9.

Discovery of biphenyl piperazines as novel and long acting muscarinic acetylcholine receptor antagonists.

Jin J, Budzik B, Wang Y, Shi D, Wang F, Xie H, Wan Z, Zhu C, Foley JJ, Webb EF, Berlanga M, Burman M, Sarau HM, Morrow DM, Moore ML, Rivero RA, Palovich M, Salmon M, Belmonte KE, Lainé DI.

J Med Chem. 2008 Oct 9;51(19):5915-8. doi: 10.1021/jm800935u. Epub 2008 Sep 18.

PMID:
18798607
10.

Discovery of novel and long acting muscarinic acetylcholine receptor antagonists.

Jin J, Wang Y, Shi D, Wang F, Davis RS, Jin Q, Fu W, Foley JJ, Webb EF, Dehaas CJ, Berlanga M, Burman M, Sarau HM, Morrow DM, Rao P, Kallal LA, Moore ML, Rivero RA, Palovich M, Salmon M, Belmonte KE, Busch-Petersen J.

J Med Chem. 2008 Aug 28;51(16):4866-9. doi: 10.1021/jm800634k. Epub 2008 Aug 5.

PMID:
18680280
11.

Urotensin-II receptor antagonists: synthesis and SAR of N-cyclic azaalkyl benzamides.

Jin J, An M, Sapienza A, Aiyar N, Naselsky D, Sarau HM, Foley JJ, Salyers KL, Knight SD, Keenan RM, Rivero RA, Dhanak D, Douglas SA.

Bioorg Med Chem Lett. 2008 Jul 15;18(14):3950-4. doi: 10.1016/j.bmcl.2008.06.019. Epub 2008 Jun 10.

PMID:
18573659
12.

3-Arylamino-2H-1,2,4-benzothiadiazin-5-ol 1,1-dioxides as novel and selective CXCR2 antagonists.

Wang Y, Busch-Petersen J, Wang F, Ma L, Fu W, Kerns JK, Jin J, Palovich MR, Shen JK, Burman M, Foley JJ, Schmidt DB, Hunsberger GE, Sarau HM, Widdowson KL.

Bioorg Med Chem Lett. 2007 Jul 15;17(14):3864-7. Epub 2007 May 10.

PMID:
17524641
13.

Oxazolidinones as novel human CCR8 antagonists.

Jin J, Wang Y, Wang F, Kerns JK, Vinader VM, Hancock AP, Lindon MJ, Stevenson GI, Morrow DM, Rao P, Nguyen C, Barrett VJ, Browning C, Hartmann G, Andrew DP, Sarau HM, Foley JJ, Jurewicz AJ, Fornwald JA, Harker AJ, Moore ML, Rivero RA, Belmonte KE, Connor HE.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1722-5. Epub 2006 Dec 24.

PMID:
17267215
14.

Comparison of N,N'-diarylsquaramides and N,N'-diarylureas as antagonists of the CXCR2 chemokine receptor.

McCleland BW, Davis RS, Palovich MR, Widdowson KL, Werner ML, Burman M, Foley JJ, Schmidt DB, Sarau HM, Rogers M, Salyers KL, Gorycki PD, Roethke TJ, Stelman GJ, Azzarano LM, Ward KW, Busch-Petersen J.

Bioorg Med Chem Lett. 2007 Mar 15;17(6):1713-7. Epub 2006 Dec 23.

PMID:
17236763
15.

N,N'-Diarylcyanoguanidines as antagonists of the CXCR2 and CXCR1 chemokine receptors.

Nie H, Widdowson KL, Palovich MR, Fu W, Elliott JD, Bryan DL, Burman M, Schmidt DB, Foley JJ, Sarau HM, Busch-Petersen J.

Bioorg Med Chem Lett. 2006 Nov 1;16(21):5513-6. Epub 2006 Aug 24.

PMID:
16934456
16.

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.

17.

A novel flow cytometric assay of human whole blood neutrophil and monocyte CD11b levels: upregulation by chemokines is related to receptor expression, comparison with neutrophil shape change, and effects of a chemokine receptor (CXCR2) antagonist.

Nicholson GC, Tennant RC, Carpenter DC, Sarau HM, Kon OM, Barnes PJ, Salmon M, Vessey RS, Tal-Singer R, Hansel TT.

Pulm Pharmacol Ther. 2007;20(1):52-9. Epub 2006 Jan 6.

PMID:
16406722
18.

Aminoalkoxybenzyl pyrrolidines as novel human urotensin-II receptor antagonists.

Jin J, Dhanak D, Knight SD, Widdowson K, Aiyar N, Naselsky D, Sarau HM, Foley JJ, Schmidt DB, Bennett CD, Wang B, Warren GL, Moore ML, Keenan RM, Rivero RA, Douglas SA.

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3229-32.

PMID:
15936190
19.

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.

20.

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
21.

Neuromedin U elicits cytokine release in murine Th2-type T cell clone D10.G4.1.

Johnson EN, Appelbaum ER, Carpenter DC, Cox RF, Disa J, Foley JJ, Ghosh SK, Naselsky DP, Pullen MA, Sarau HM, Scheff SR, Steplewski KM, Zaks-Zilberman M, Aiyar N.

J Immunol. 2004 Dec 15;173(12):7230-8.

22.

A synthetic, non-peptide CXCR2 antagonist blocks MIP-2-induced neutrophil migration in mice.

Matzer SP, Zombou J, Sarau HM, Röllinghoff M, Beuscher HU.

Immunobiology. 2004;209(3):225-33.

PMID:
15518334
23.

A coding polymorphism in the CYSLT2 receptor with reduced affinity to LTD4 is associated with asthma.

Pillai SG, Cousens DJ, Barnes AA, Buckley PT, Chiano MN, Hosking LK, Cameron LA, Fling ME, Foley JJ, Green A, Sarau HM, Schmidt DB, Sprankle CS, Blumenthal MN, Vestbo J, Kennedy-Wilson K, Wixted WE, Wagner MJ, Anderson WH, Ignar DM; Investigators of the GAIN Network.

Pharmacogenetics. 2004 Sep;14(9):627-33.

PMID:
15475736
24.

Discovery of potent and orally bioavailable N,N'-diarylurea antagonists for the CXCR2 chemokine receptor.

Jin Q, Nie H, McCleland BW, Widdowson KL, Palovich MR, Elliott JD, Goodman RM, Burman M, Sarau HM, Ward KW, Nord M, Orr BM, Gorycki PD, Busch-Petersen J.

Bioorg Med Chem Lett. 2004 Sep 6;14(17):4375-8.

PMID:
15357956
25.

Radioligand binding and functional characterization of recombinant human NmU1 and NmU2 receptors stably expressed in clonal human embryonic kidney-293 cells.

Aiyar N, Disa J, Foley JJ, Buckley PT, Wixted WE, Pullen M, Shabon U, Dul E, Szekeres PG, Elshourbagy NA, Sarau HM, Appelbaum E, Bolaky J.

Pharmacology. 2004 Sep;72(1):33-41.

PMID:
15292653
26.

Localisation of NMU1R and NMU2R in human and rat central nervous system and effects of neuromedin-U following central administration in rats.

Gartlon J, Szekeres P, Pullen M, Sarau HM, Aiyar N, Shabon U, Michalovich D, Steplewski K, Ellis C, Elshourbagy N, Duxon M, Ashmeade TE, Harrison DC, Murdock P, Wilson S, Ennaceur A, Atkins A, Heidbreder C, Hagan JJ, Hunter AJ, Jones DN.

Psychopharmacology (Berl). 2004 Dec;177(1-2):1-14. Epub 2004 Jun 16.

PMID:
15205870
27.

Evaluation of potent and selective small-molecule antagonists for the CXCR2 chemokine receptor.

Widdowson KL, Elliott JD, Veber DF, Nie H, Rutledge MC, McCleland BW, Xiang JN, Jurewicz AJ, Hertzberg RP, Foley JJ, Griswold DE, Martin L, Lee JM, White JR, Sarau HM.

J Med Chem. 2004 Mar 11;47(6):1319-21.

PMID:
14998320
28.

Regulation of TNF-alpha- and IFN-gamma-induced CXCL10 expression: participation of the airway smooth muscle in the pulmonary inflammatory response in chronic obstructive pulmonary disease.

Hardaker EL, Bacon AM, Carlson K, Roshak AK, Foley JJ, Schmidt DB, Buckley PT, Comegys M, Panettieri RA Jr, Sarau HM, Belmonte KE.

FASEB J. 2004 Jan;18(1):191-3. Epub 2003 Nov 3.

PMID:
14597565
29.

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.

30.

Chemokine-cytokine cross-talk. The ELR+ CXC chemokine LIX (CXCL5) amplifies a proinflammatory cytokine response via a phosphatidylinositol 3-kinase-NF-kappa B pathway.

Chandrasekar B, Melby PC, Sarau HM, Raveendran M, Perla RP, Marelli-Berg FM, Dulin NO, Singh IS.

J Biol Chem. 2003 Feb 14;278(7):4675-86. Epub 2002 Dec 4.

31.

A potent and selective nonpeptide antagonist of CXCR2 inhibits acute and chronic models of arthritis in the rabbit.

Podolin PL, Bolognese BJ, Foley JJ, Schmidt DB, Buckley PT, Widdowson KL, Jin Q, White JR, Lee JM, Goodman RB, Hagen TR, Kajikawa O, Marshall LA, Hay DW, Sarau HM.

J Immunol. 2002 Dec 1;169(11):6435-44.

32.

Nonpeptide tachykinin receptor antagonists. III. SB 235375, a low central nervous system-penetrant, potent and selective neurokinin-3 receptor antagonist, inhibits citric acid-induced cough and airways hyper-reactivity in guinea pigs.

Hay DW, Giardina GA, Griswold DE, Underwood DC, Kotzer CJ, Bush B, Potts W, Sandhu P, Lundberg D, Foley JJ, Schmidt DB, Martin LD, Kilian D, Legos JJ, Barone FC, Luttmann MA, Grugni M, Raveglia LF, Sarau HM.

J Pharmacol Exp Ther. 2002 Jan;300(1):314-23.

PMID:
11752131
33.

Cloning, pharmacology, and tissue distribution of G-protein-coupled receptor GPR105 (KIAA0001) rodent orthologs.

Freeman K, Tsui P, Moore D, Emson PC, Vawter L, Naheed S, Lane P, Bawagan H, Herrity N, Murphy K, Sarau HM, Ames RS, Wilson S, Livi GP, Chambers JK.

Genomics. 2001 Dec;78(3):124-8.

PMID:
11735218
34.

Interleukin-8 receptor antagonists in pulmonary diseases.

Hay DW, Sarau HM.

Curr Opin Pharmacol. 2001 Jun;1(3):242-7. Review.

PMID:
11712746
35.

EDG1 receptor stimulation leads to cardiac hypertrophy in rat neonatal myocytes.

Robert P, Tsui P, Laville MP, Livi GP, Sarau HM, Bril A, Berrebi-Bertrand I.

J Mol Cell Cardiol. 2001 Sep;33(9):1589-606.

PMID:
11549339
36.

AXOR12, a novel human G protein-coupled receptor, activated by the peptide KiSS-1.

Muir AI, Chamberlain L, Elshourbagy NA, Michalovich D, Moore DJ, Calamari A, Szekeres PG, Sarau HM, Chambers JK, Murdock P, Steplewski K, Shabon U, Miller JE, Middleton SE, Darker JG, Larminie CG, Wilson S, Bergsma DJ, Emson P, Faull R, Philpott KL, Harrison DC.

J Biol Chem. 2001 Aug 3;276(31):28969-75. Epub 2001 May 31.

37.

Discovery of potent and selective phenylalanine derived CCR3 receptor antagonists. Part 2.

Dhanak D, Christmann LT, Darcy MG, Keenan RM, Knight SD, Lee J, Ridgers LH, Sarau HM, Shah DH, White JR, Zhang L.

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1445-50.

PMID:
11378374
38.

Discovery of potent and selective phenylalanine derived CCR3 antagonists. Part 1.

Dhanak D, Christmann LT, Darcy MG, Jurewicz AJ, Keenan RM, Lee J, Sarau HM, Widdowson KL, White JR.

Bioorg Med Chem Lett. 2001 Jun 4;11(11):1441-4.

PMID:
11378373
39.

Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists.

Blaney FE, Raveglia LF, Artico M, Cavagnera S, Dartois C, Farina C, Grugni M, Gagliardi S, Luttmann MA, Martinelli M, Nadler GM, Parini C, Petrillo P, Sarau HM, Scheideler MA, Hay DW, Giardina GA.

J Med Chem. 2001 May 24;44(11):1675-89.

PMID:
11356103
40.

Identification of a selective nonpeptide antagonist of the anaphylatoxin C3a receptor that demonstrates antiinflammatory activity in animal models.

Ames RS, Lee D, Foley JJ, Jurewicz AJ, Tornetta MA, Bautsch W, Settmacher B, Klos A, Erhard KF, Cousins RD, Sulpizio AC, Hieble JP, McCafferty G, Ward KW, Adams JL, Bondinell WE, Underwood DC, Osborn RR, Badger AM, Sarau HM.

J Immunol. 2001 May 15;166(10):6341-8.

41.

Molecular and pharmacological characterization of the murine tachykinin NK(3) receptor.

Sarau HM, Feild JA, Ames RS, Foley JJ, Nuthulaganti P, Schmidt DB, Buckley PT, Elshourbagy NA, Brawner ME, Luttmann MA, Giardina GA, Hay DW.

Eur J Pharmacol. 2001 Feb 16;413(2-3):143-50.

PMID:
11226387
42.

Cloning, expression, and pharmacological characterization of a novel human histamine receptor.

Zhu Y, Michalovich D, Wu H, Tan KB, Dytko GM, Mannan IJ, Boyce R, Alston J, Tierney LA, Li X, Herrity NC, Vawter L, Sarau HM, Ames RS, Davenport CM, Hieble JP, Wilson S, Bergsma DJ, Fitzgerald LR.

Mol Pharmacol. 2001 Mar;59(3):434-41.

PMID:
11179436
43.

A G protein-coupled receptor for UDP-glucose.

Chambers JK, Macdonald LE, Sarau HM, Ames RS, Freeman K, Foley JJ, Zhu Y, McLaughlin MM, Murdock P, McMillan L, Trill J, Swift A, Aiyar N, Taylor P, Vawter L, Naheed S, Szekeres P, Hervieu G, Scott C, Watson JM, Murphy AJ, Duzic E, Klein C, Bergsma DJ, Wilson S, Livi GP.

J Biol Chem. 2000 Apr 14;275(15):10767-71.

44.

Calmodulin-binding peptide PEP-19 modulates activation of calmodulin kinase II In situ.

Johanson RA, Sarau HM, Foley JJ, Slemmon JR.

J Neurosci. 2000 Apr 15;20(8):2860-6.

45.

Differential vasoconstrictor activity of human urotensin-II in vascular tissue isolated from the rat, mouse, dog, pig, marmoset and cynomolgus monkey.

Douglas SA, Sulpizio AC, Piercy V, Sarau HM, Ames RS, Aiyar NV, Ohlstein EH, Willette RN.

Br J Pharmacol. 2000 Dec;131(7):1262-74.

46.

Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist.

Sarau HM, Griswold DE, Bush B, Potts W, Sandhu P, Lundberg D, Foley JJ, Schmidt DB, Webb EF, Martin LD, Legos JJ, Whitmore RG, Barone FC, Medhurst AD, Luttmann MA, Giardina GA, Hay DW.

J Pharmacol Exp Ther. 2000 Oct;295(1):373-81.

PMID:
10992004
47.

Identification of potent, selective non-peptide CC chemokine receptor-3 antagonist that inhibits eotaxin-, eotaxin-2-, and monocyte chemotactic protein-4-induced eosinophil migration.

White JR, Lee JM, Dede K, Imburgia CS, Jurewicz AJ, Chan G, Fornwald JA, Dhanak D, Christmann LT, Darcy MG, Widdowson KL, Foley JJ, Schmidt DB, Sarau HM.

J Biol Chem. 2000 Nov 24;275(47):36626-31.

48.

Evidence that the proposed novel human "neurokinin-4" receptor is pharmacologically similar to the human neurokinin-3 receptor but is not of human origin.

Sarau HM, Mooney JL, Schmidt DB, Foley JJ, Buckley PT, Giardina GA, Wang DY, Lee JA, Hay DW.

Mol Pharmacol. 2000 Sep;58(3):552-9.

PMID:
10953048
49.

Identification of an EDG7 variant, HOFNH30, a G-protein-coupled receptor for lysophosphatidic acid.

Fitzgerald LR, Dytko GM, Sarau HM, Mannan IJ, Ellis C, Lane PA, Tan KB, Murdock PR, Wilson S, Bergsma DJ, Ames RS, Foley JJ, Campbell DA, McMillan L, Evans N, Elshourbagy NA, Minehart H, Tsui P.

Biochem Biophys Res Commun. 2000 Jul 14;273(3):805-10.

PMID:
10891327
50.

Receptor for the pain modulatory neuropeptides FF and AF is an orphan G protein-coupled receptor.

Elshourbagy NA, Ames RS, Fitzgerald LR, Foley JJ, Chambers JK, Szekeres PG, Evans NA, Schmidt DB, Buckley PT, Dytko GM, Murdock PR, Milligan G, Groarke DA, Tan KB, Shabon U, Nuthulaganti P, Wang DY, Wilson S, Bergsma DJ, Sarau HM.

J Biol Chem. 2000 Aug 25;275(34):25965-71.

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