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Items: 1 to 50 of 139

1.

Selective Prostacyclin Receptor Agonist Selexipag, in Contrast to Prostacyclin Analogs, Does Not Evoke Paradoxical Vasoconstriction of the Rat Femoral Artery.

Morrison K, Haag F, Ernst R, Iglarz M, Clozel M.

J Pharmacol Exp Ther. 2018 Jun;365(3):727-733. doi: 10.1124/jpet.117.246058. Epub 2018 Mar 27.

PMID:
29588339
2.

Cenerimod, a novel selective S1P1 receptor modulator with unique signaling properties.

Piali L, Birker-Robaczewska M, Lescop C, Froidevaux S, Schmitz N, Morrison K, Kohl C, Rey M, Studer R, Vezzali E, Hess P, Clozel M, Steiner B, Bolli MH, Nayler O.

Pharmacol Res Perspect. 2017 Dec;5(6). doi: 10.1002/prp2.370.

3.

The reversible P2Y12 antagonist ACT-246475 causes significantly less blood loss than ticagrelor at equivalent antithrombotic efficacy in rat.

Rey M, Kramberg M, Hess P, Morrison K, Ernst R, Haag F, Weber E, Clozel M, Baumann M, Caroff E, Hubler F, Riederer MA, Steiner B.

Pharmacol Res Perspect. 2017 Oct;5(5). doi: 10.1002/prp2.338.

4.

Selexipag Active Metabolite ACT-333679 Displays Strong Anticontractile and Antiremodeling Effects but Low β-Arrestin Recruitment and Desensitization Potential.

Gatfield J, Menyhart K, Wanner D, Gnerre C, Monnier L, Morrison K, Hess P, Iglarz M, Clozel M, Nayler O.

J Pharmacol Exp Ther. 2017 Jul;362(1):186-199. doi: 10.1124/jpet.116.239665. Epub 2017 May 5.

5.

Endothelin ETA Receptor Blockade, by Activating ETB Receptors, Increases Vascular Permeability and Induces Exaggerated Fluid Retention.

Vercauteren M, Trensz F, Pasquali A, Cattaneo C, Strasser DS, Hess P, Iglarz M, Clozel M.

J Pharmacol Exp Ther. 2017 May;361(2):322-333. doi: 10.1124/jpet.116.234930. Epub 2017 Feb 21.

6.

Characterization of Novel Antimalarial Compound ACT-451840: Preclinical Assessment of Activity and Dose-Efficacy Modeling.

Le Bihan A, de Kanter R, Angulo-Barturen I, Binkert C, Boss C, Brun R, Brunner R, Buchmann S, Burrows J, Dechering KJ, Delves M, Ewerling S, Ferrer S, Fischli C, Gamo-Benito FJ, Gnädig NF, Heidmann B, Jiménez-Díaz MB, Leroy D, Martínez MS, Meyer S, Moehrle JJ, Ng CL, Noviyanti R, Ruecker A, Sanz LM, Sauerwein RW, Scheurer C, Schleiferboeck S, Sinden R, Snyder C, Straimer J, Wirjanata G, Marfurt J, Price RN, Weller T, Fischli W, Fidock DA, Clozel M, Wittlin S.

PLoS Med. 2016 Oct 4;13(10):e1002138. doi: 10.1371/journal.pmed.1002138. eCollection 2016 Oct.

7.

Endothelin research and the discovery of macitentan for the treatment of pulmonary arterial hypertension.

Clozel M.

Am J Physiol Regul Integr Comp Physiol. 2016 Oct 1;311(4):R721-R726. doi: 10.1152/ajpregu.00475.2015. Epub 2016 Aug 17. Review.

8.

CRISPR-Cas9-modified pfmdr1 protects Plasmodium falciparum asexual blood stages and gametocytes against a class of piperazine-containing compounds but potentiates artemisinin-based combination therapy partner drugs.

Ng CL, Siciliano G, Lee MC, de Almeida MJ, Corey VC, Bopp SE, Bertuccini L, Wittlin S, Kasdin RG, Le Bihan A, Clozel M, Winzeler EA, Alano P, Fidock DA.

Mol Microbiol. 2016 Aug;101(3):381-93. doi: 10.1111/mmi.13397. Epub 2016 May 7.

9.

Cadazolid Does Not Promote Intestinal Colonization of Vancomycin-Resistant Enterococci in Mice.

Seiler P, Enderlin-Paput M, Pfaff P, Weiss M, Ritz D, Clozel M, Locher HH.

Antimicrob Agents Chemother. 2015 Oct 26;60(1):628-31. doi: 10.1128/AAC.01923-15. Print 2016 Jan.

10.

Selexipag: An Oral and Selective IP Prostacyclin Receptor Agonist for the Treatment of Pulmonary Arterial Hypertension.

Asaki T, Kuwano K, Morrison K, Gatfield J, Hamamoto T, Clozel M.

J Med Chem. 2015 Sep 24;58(18):7128-37. doi: 10.1021/acs.jmedchem.5b00698. Epub 2015 Sep 16.

PMID:
26291199
11.

Development of macitentan for the treatment of pulmonary arterial hypertension.

Selej M, Romero AJ, Channick RN, Clozel M.

Ann N Y Acad Sci. 2015 Nov;1358:68-81. doi: 10.1111/nyas.12856. Epub 2015 Aug 20. Review.

PMID:
26291180
12.

Comparison of Macitentan and Bosentan on Right Ventricular Remodeling in a Rat Model of Non-vasoreactive Pulmonary Hypertension.

Iglarz M, Landskroner K, Bauer Y, Vercauteren M, Rey M, Renault B, Studer R, Vezzali E, Freti D, Hadana H, Schläpfer M, Cattaneo C, Bortolamiol C, Weber E, Whitby BR, Delahaye S, Wanner D, Steiner P, Nayler O, Hess P, Clozel M.

J Cardiovasc Pharmacol. 2015 Nov;66(5):457-67. doi: 10.1097/FJC.0000000000000296.

13.

Vascular Effects of Endothelin Receptor Antagonists Depends on Their Selectivity for ETA Versus ETB Receptors and on the Functionality of Endothelial ETB Receptors.

Iglarz M, Steiner P, Wanner D, Rey M, Hess P, Clozel M.

J Cardiovasc Pharmacol. 2015 Oct;66(4):332-7. doi: 10.1097/FJC.0000000000000283.

14.

Comparison of pharmacological activity of macitentan and bosentan in preclinical models of systemic and pulmonary hypertension.

Iglarz M, Bossu A, Wanner D, Bortolamiol C, Rey M, Hess P, Clozel M.

Life Sci. 2014 Nov 24;118(2):333-9. doi: 10.1016/j.lfs.2014.02.018. Epub 2014 Feb 26.

15.

Therapeutic use of a selective S1P1 receptor modulator ponesimod in autoimmune diabetes.

You S, Piali L, Kuhn C, Steiner B, Sauvaget V, Valette F, Clozel M, Bach JF, Chatenoud L.

PLoS One. 2013 Oct 24;8(10):e77296. doi: 10.1371/journal.pone.0077296. eCollection 2013.

16.

Endothelin receptor antagonists.

Clozel M, Maresta A, Humbert M.

Handb Exp Pharmacol. 2013;218:199-227. doi: 10.1007/978-3-642-38664-0_9. Review.

PMID:
24092342
17.

Desensitization by progressive up-titration prevents first-dose effects on the heart: guinea pig study with ponesimod, a selective S1P1 receptor modulator.

Rey M, Hess P, Clozel M, Delahaye S, Gatfield J, Nayler O, Steiner B.

PLoS One. 2013 Sep 12;8(9):e74285. doi: 10.1371/journal.pone.0074285. eCollection 2013.

18.

Slow receptor dissociation kinetics differentiate macitentan from other endothelin receptor antagonists in pulmonary arterial smooth muscle cells.

Gatfield J, Mueller Grandjean C, Sasse T, Clozel M, Nayler O.

PLoS One. 2012;7(10):e47662. doi: 10.1371/journal.pone.0047662. Epub 2012 Oct 15.

19.

Differential effects of Selexipag [corrected] and prostacyclin analogs in rat pulmonary artery.

Morrison K, Studer R, Ernst R, Haag F, Kauser K, Clozel M.

J Pharmacol Exp Ther. 2012 Dec;343(3):547-55. doi: 10.1124/jpet.112.197152. Epub 2012 Aug 23. Erratum in: J Pharmacol Exp Ther. 2013 Jan;344(1):317.

20.

The discovery of N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N'-propylsulfamide (Macitentan), an orally active, potent dual endothelin receptor antagonist.

Bolli MH, Boss C, Binkert C, Buchmann S, Bur D, Hess P, Iglarz M, Meyer S, Rein J, Rey M, Treiber A, Clozel M, Fischli W, Weller T.

J Med Chem. 2012 Sep 13;55(17):7849-61. doi: 10.1021/jm3009103. Epub 2012 Aug 16.

PMID:
22862294
21.

Identification of cathepsin L as a potential sex-specific biomarker for renal damage.

Bauer Y, Hess P, Qiu C, Klenk A, Renault B, Wanner D, Studer R, Killer N, Stalder AK, Stritt M, Strasser DS, Farine H, Kauser K, Clozel M, Fischli W, Nayler O.

Hypertension. 2011 Apr;57(4):795-801. doi: 10.1161/HYPERTENSIONAHA.110.157206. Epub 2011 Feb 28.

PMID:
21357272
22.

The selective sphingosine 1-phosphate receptor 1 agonist ponesimod protects against lymphocyte-mediated tissue inflammation.

Piali L, Froidevaux S, Hess P, Nayler O, Bolli MH, Schlosser E, Kohl C, Steiner B, Clozel M.

J Pharmacol Exp Ther. 2011 May;337(2):547-56. doi: 10.1124/jpet.110.176487. Epub 2011 Feb 23.

23.

Between confidentiality and scientific exchange: the place of publication in drug discovery and pharmaceutical research.

Clozel M.

Sci Transl Med. 2011 Jan 26;3(67):67cm2. doi: 10.1126/scitranslmed.3001890.

PMID:
21270337
24.

The cardiovascular physiology and pharmacology of endothelin-1.

Thorin E, Clozel M.

Adv Pharmacol. 2010;60:1-26. doi: 10.1016/B978-0-12-385061-4.00001-5. Review.

25.

At the heart of tissue: endothelin system and end-organ damage.

Iglarz M, Clozel M.

Clin Sci (Lond). 2010 Aug 17;119(11):453-63. doi: 10.1042/CS20100222. Review.

PMID:
20712600
26.

Selexipag: a selective prostacyclin receptor agonist that does not affect rat gastric function.

Morrison K, Ernst R, Hess P, Studer R, Clozel M.

J Pharmacol Exp Ther. 2010 Oct;335(1):249-55. doi: 10.1124/jpet.110.169748. Epub 2010 Jul 21.

27.

Monocrotaline-induced pulmonary hypertension in Wistar rats.

Rey M, Hess P, Clozel M.

Curr Protoc Pharmacol. 2009 Sep;Chapter 5:Unit 5.56. doi: 10.1002/0471141755.ph0556s46.

PMID:
22294402
28.

Tezosentan, a novel endothelin receptor antagonist, markedly reduces rat hepatic ischemia and reperfusion injury in three different models.

Farmer DG, Kaldas F, Anselmo D, Katori M, Shen XD, Lassman C, Kaldas M, Clozel M, Busuttil RW, Kupiec-Weglinski J.

Liver Transpl. 2008 Dec;14(12):1737-44. doi: 10.1002/lt.21621.

29.

Pharmacology of macitentan, an orally active tissue-targeting dual endothelin receptor antagonist.

Iglarz M, Binkert C, Morrison K, Fischli W, Gatfield J, Treiber A, Weller T, Bolli MH, Boss C, Buchmann S, Capeleto B, Hess P, Qiu C, Clozel M.

J Pharmacol Exp Ther. 2008 Dec;327(3):736-45. doi: 10.1124/jpet.108.142976. Epub 2008 Sep 9.

30.

Mechanisms of ET-1-induced endothelial dysfunction.

Iglarz M, Clozel M.

J Cardiovasc Pharmacol. 2007 Dec;50(6):621-8. Review.

PMID:
18091577
31.
32.
33.

Promotion of sleep by targeting the orexin system in rats, dogs and humans.

Brisbare-Roch C, Dingemanse J, Koberstein R, Hoever P, Aissaoui H, Flores S, Mueller C, Nayler O, van Gerven J, de Haas SL, Hess P, Qiu C, Buchmann S, Scherz M, Weller T, Fischli W, Clozel M, Jenck F.

Nat Med. 2007 Feb;13(2):150-5. Epub 2007 Jan 28.

PMID:
17259994
34.

Endothelin-1/endothelin-3 ratio: a potential prognostic factor of pulmonary arterial hypertension.

Montani D, Souza R, Binkert C, Fischli W, Simonneau G, Clozel M, Humbert M.

Chest. 2007 Jan;131(1):101-8.

PMID:
17218562
35.

A phase II study of bosentan, a dual endothelin receptor antagonist, as monotherapy in patients with stage IV metastatic melanoma.

Kefford R, Beith JM, Van Hazel GA, Millward M, Trotter JM, Wyld DK, Kusic R, Shreeniwas R, Morganti A, Ballmer A, Segal E, Nayler O, Clozel M.

Invest New Drugs. 2007 Jun;25(3):247-52. Epub 2006 Oct 5.

PMID:
17021960
36.

Bosentan, sildenafil, and their combination in the monocrotaline model of pulmonary hypertension in rats.

Clozel M, Hess P, Rey M, Iglarz M, Binkert C, Qiu C.

Exp Biol Med (Maywood). 2006 Jun;231(6):967-73.

PMID:
16741032
37.

The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats.

Clozel M, Hess P, Qiu C, Ding SS, Rey M.

J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21. Epub 2005 Nov 2.

38.
39.

The pharmacology of bosentan.

Breu V, Ertel SI, Roux S, Clozel M.

Expert Opin Investig Drugs. 1998 Jul;7(7):1173-92.

PMID:
15992023
40.

Role of endothelin in fibrosis and anti-fibrotic potential of bosentan.

Clozel M, Salloukh H.

Ann Med. 2005;37(1):2-12. Review.

PMID:
15902842
41.

Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System.

Clozel M, Binkert C, Birker-Robaczewska M, Boukhadra C, Ding SS, Fischli W, Hess P, Mathys B, Morrison K, Müller C, Müller C, Nayler O, Qiu C, Rey M, Scherz MW, Velker J, Weller T, Xi JF, Ziltener P.

J Pharmacol Exp Ther. 2004 Oct;311(1):204-12. Epub 2004 May 14.

42.

Novel benzo[1,4]diazepin-2-one derivatives as endothelin receptor antagonists.

Bolli MH, Marfurt J, Grisostomi C, Boss C, Binkert C, Hess P, Treiber A, Thorin E, Morrison K, Buchmann S, Bur D, Ramuz H, Clozel M, Fischli W, Weller T.

J Med Chem. 2004 May 20;47(11):2776-95.

PMID:
15139756
44.

Role of endothelin-1 and thromboxane A2 in the pulmonary hypertension induced by heparin-protamine interaction in anesthetized dogs.

Freitas CF, Faro R, Dragosavac D, Clozel M, De Nucci G, Antunes E.

J Cardiovasc Pharmacol. 2004 Jan;43(1):106-12.

PMID:
14668575
45.
46.

Chronic endothelin receptor blockade prevents both early hyperfiltration and late overt diabetic nephropathy in the rat.

Ding SS, Qiu C, Hess P, Xi JF, Zheng N, Clozel M.

J Cardiovasc Pharmacol. 2003 Jul;42(1):48-54.

PMID:
12827026
47.

The use of sulfonylamido pyrimidines incorporating an unsaturated side chain as endothelin receptor antagonists.

Bolli MH, Boss C, Clozel M, Fischli W, Hess P, Weller T.

Bioorg Med Chem Lett. 2003 Mar 10;13(5):955-9.

PMID:
12617929
48.

Bis-sulfonamides as endothelin receptor antagonists.

Boss C, Bolli MH, Weller T, Fischli W, Clozel M.

Bioorg Med Chem Lett. 2003 Mar 10;13(5):951-4.

PMID:
12617928
49.

Combination of low-dose valsartan and enalapril improves endothelial dysfunction and coronary reserve in Nomega-nitro-L-arginine methyl ester-treated spontaneously hypertensive rats.

de Gasparo M, Hess P, Clozel M, Persohn E, Roman D, Germann PG, Clozel JP, Webb RL.

J Cardiovasc Pharmacol. 2002 Nov;40(5):789-800.

PMID:
12409988
50.

Entry-into-humans study with tezosentan, an intravenous dual endothelin receptor antagonist.

Dingemanse J, Clozel M, van Giersbergen PL.

J Cardiovasc Pharmacol. 2002 Jun;39(6):795-802.

PMID:
12021573

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