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Akademický článek

Milestones to the Discovery of T-type Calcium Channel Blockers for the Treatment of Generalized Epilepsies

Publikováno v: CHIMIA, Vol 71, Iss 10 (2017)

We describe the discovery and optimization of new, brain-penetrant T-type calcium channel blockers. We present optimized compounds with excellent efficacy in a rodent model of generalized absence-like epilepsy. Along the fine optimization of a chemic

Externí odkaz: https://doaj.org/article/77760779eafd425e854518b6109e1f36

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The P2Y12 Receptor Antagonist Selatogrel Dissolves Preformed Platelet Thrombi In Vivo

Autor: Martine Baumann, Laurence Panicot-Dubois, Markus Rey, Sébastien Roux, Markus A. Riederer, Lydie Crescence, Christophe Dubois, Markus Kramberg

Publikováno v: Journal of Clinical Medicine
Journal of Clinical Medicine, 2021, 10 (22), pp.5349. ⟨10.3390/jcm10225349⟩
Journal of Clinical Medicine, Vol 10, Iss 5349, p 5349 (2021)
Volume 10
Issue 22

Selatogrel, a potent and reversible antagonist of the P2Y12 receptor, inhibited FeCl3-induced thrombosis in rats. Here, we report the anti-thrombotic effect of selatogrel after subcutaneous applications in guinea pigs and mice. Selatogrel inhibited p

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d96b3b0eea1541cef6fdf1ba86b3761
https://amu.hal.science/hal-03653449

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Pharmacological Characterization of Aprocitentan, a Dual Endothelin Receptor Antagonist, Alone and in Combination with Blockers of the Renin Angiotensin System, in Two Models of Experimental Hypertension

Autor: Ulrich Mentzel, Markus Kramberg, Marc Iglarz, Enrico Vezzali, Frederic Trensz, Céline Bortolamiol, Daniel Wanner, Stephane Delahaye, Hakim Hadana, Daniel S. Strasser, Patrick Hess, Markus Rey, Joël Ménard, Martine Clozel

Publikováno v: Journal of Pharmacology and Experimental Therapeutics. 368:462-473

The endothelin (ET) system has emerged as a novel target for hypertension treatment where a medical need persists despite availability of several pharmacological classes, including renin angiotensin system (RAS) blockers. ET receptor antagonism has d

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4d32d8d86285b9758185f4b07108c406
https://doi.org/10.1124/jpet.118.253864

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Monetarisierung von maschinengenerierten Onlinedaten – Branchenübergreifende Chancen und Herausforderungen

Autor: Nathalie Huber, Markus Rey, Thorsten Beule, Malte Brettel

Publikováno v: Monetarisierung von technischen Daten ISBN: 9783662629147

Unternehmen konnen in der heutigen Zeit mithilfe von fortgeschrittenen Formen der Datenanalyse Erkenntnisse erzielen, die sich unmittelbar in Wettbewerbsvorteile umsetzen lassen. Ermoglicht wird dies insbesondere durch eine exponentiell zunehmende Me

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::8914373ff81a2ba39c3f3b28849efca6
https://doi.org/10.1007/978-3-662-62915-4_6

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Akademický článek

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

Autor: Markus Rey, Patrick Hess, Martine Clozel, Stéphane Delahaye, John Gatfield, Oliver Nayler, Beat Steiner

Publikováno v: PLoS ONE, Vol 8, Iss 9, p e74285 (2013)

Ponesimod, a selective S1P1 receptor modulator, reduces the blood lymphocyte count in all tested species by preventing egress of T and B cells from thymus and peripheral lymphoid organs. In addition, ponesimod transiently affects heart rate and atrio

Externí odkaz: https://doaj.org/article/d79ad88e62a94ce89ceedd137f337bd6

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S1P1 Modulator-Induced Gαi Signaling and β-Arrestin Recruitment Are Both Necessary to Induce Rapid and Efficient Reduction of Blood Lymphocyte Count In Vivo

Autor: Christopher Kohl, Markus Rey, Ruben de Kanter, Cyrille Lescop, Maxime Boucher, Magdalena Birker-Robaczewska, Oliver Nayler, Martin Bolli, Sylvie Poirey, Beat Steiner

Publikováno v: Molecular Pharmacology. 93:109-118

S1P1 (sphingosine-1-phosphate receptor 1) agonists prevent lymphocyte egress from secondary lymphoid organs and cause a reduction in the number of circulating blood lymphocytes. We hypothesized that S1P1 receptor modulators with pathway-selective sig

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::03caf535b0e0a5e2166c0797fdb6a500
https://doi.org/10.1124/mol.117.109140

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Preparation, Antiepileptic Activity, and Cardiovascular Safety of Dihydropyrazoles as Brain-Penetrant T-Type Calcium Channel Blockers

Autor: Melanie Kessler, Eric A. Ertel, John Gatfield, Rick D Gaston, Corinna Grisostomi, Thomas Pfeifer, Lubos Remen, Lloyd Simons, Olivier Bezencon, Johannes Mosbacher, Catherine Roch, Richard Moon, Dennis Michael Downing, Markus Rey

Publikováno v: Journal of Medicinal Chemistry. 59:8398-8411

A series of dihydropyrazole derivatives was developed as potent, selective, and brain-penetrating T-type calcium channel blockers. An optimized derivative, compound 6c, was advanced to in vivo studies, where it demonstrated efficacy in the WAG/Rij ra

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::4f1d15b224e97575ffd39760a63e490e
https://doi.org/10.1021/acs.jmedchem.6b00756

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Novel S1P 1 receptor agonists – Part 4: Alkylaminomethyl substituted aryl head groups

Autor: Thomas Weller, Martin Bolli, Claus Müller, Ruben de Kanter, Markus Rey, Magdalena Birker, Patrick Sieber, Cyrille Lescop, Christopher Kohl, Boris Mathys, Beat Steiner, Patrick Hess, Oliver Nayler

Publikováno v: European Journal of Medicinal Chemistry. 116:222-238

In a previous communication we reported on the discovery of alkylamino pyridine derivatives (e.g. 1) as a new class of potent, selective and efficacious S1P1 receptor (S1PR1) agonists. However, more detailed profiling revealed that this compound clas

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::6dc8392021bea5d4bf4ef196324d4ad8
https://doi.org/10.1016/j.ejmech.2016.03.048

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