Roland Ernst

CCDC 2248014: Experimental Crystal Structure Determination

François Baur, David A. Beattie, David Beer, David Bentley et autres

An entry from the Cambridge Structural Database, the world’s repository for small molecule crystal structures. The entry contains experimental data from a crystal diffraction study. The deposited dataset for this entry is freely available from the CCDC and typically includes 3D coordinates, …

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

Keith Morrison, Franck Haag, Roland Ernst, Marc Iglarz et autres

Selexipag [2-{4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy}- N -(methylsulfonyl)acetamide] is a selective nonprostanoid prostacyclin (PGI 2 ) receptor (IP receptor) agonist that is approved for the treatment of pulmonary arterial hypertension (PAH). In contrast to selexipag, PGI 2 analogs used in the clinic are nonselective agonists at …

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The reversible P2Y12antagonist ACT‐246475 causes significantly less blood loss than ticagrelor at equivalent antithrombotic efficacy in rat

Markus Rey, Markus Kramberg, Patrick Hess, Keith Morrison et autres

Abstract The P2Y12receptor is a validated target for prevention of major adverse cardiovascular events in patients with acute coronary syndrome. The aim of this study was to compare two direct‐acting, reversible P2Y12antagonists,ACT‐246475 and ticagrelor, in a rat thrombosis model by simultaneous quantification …

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Abstract 13829: The Active Metabolite of Selexipag Relaxes Rat Pulmonary Artery via Selective Activation of IP Prostacyclin Receptors

Keith Morrison, Roland Ernst, Franck Haag, Daniel Bur et autres

Introduction: Selexipag is a selective IP prostacyclin receptor agonist in development for the treatment of pulmonary arterial hypertension. Preclinical studies demonstrate that selexipag and its active metabolite ACT-333679 relax rat extralobar pulmonary artery (EPA) ex vivo . It has been reported that …

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Increased Muscle Force Production and Bone Mineral Density in ActRIIB-Fc-Treated Mature Rodents

C.-S. Chiu, Norbert Peekhaus, Hans Weber, Sharon Adamski et autres

Myostatin is a highly conserved member of the transforming growth factor-β ligand family known to regulate muscle growth via activation of activin receptors. A fusion protein consisting of the extracellular ligand-binding domain of activin type IIB receptor with the Fc portion of …

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Differential Effects of Selexipag and Prostacyclin Analogs in Rat Pulmonary Artery

Keith Morrison, R. O. Studer, Roland Ernst, Franck Haag et autres

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Selexipag: A Selective Prostacyclin Receptor Agonist that Does Not Affect Rat Gastric Function

Keith Morrison, Roland Ernst, Patrick Hess, R. O. Studer et autres

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The Identification of Indacaterol as an Ultralong-Acting Inhaled β2-Adrenoceptor Agonist

François Baur, David T. Beattie, David Beer, David Bentley et autres

Following a lipophilicity-based hypothesis, an 8-hydroxyquinolinone 2-aminoindan derived series of beta(2)-adrenoceptor agonists have been prepared and evaluated for their potential as inhaled ultralong-acting bronchodilators. Determination of their activities at the human beta(2)-adrenoceptor receptor showed symmetrical substitution of the 2-aminoindan moiety at the …

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Opioid effects on electrically-induced vasodilatation and on flare reactions in the pig's skin

L. Barthó, Roland Ernst, Fr.-K. Pierau, H. Sann

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Peripheral effect of an opioid agonist and indirect evidence for an action of an endogenous opioid on antidromic vasodilation in the pig's skin

L Barth, Roland Ernst, Fr.-K. Pierau, H. Sann

The kinetics of four 11C-labelled enkephalin peptides: Tyr-Gly-Gly-Phe-Met (Met-enkephalin), Tyr-d-Met-Gly-Phe-Pro-NH2 ((d-Met2,Pro5)-enkephalinamide), Tyr-d-Ala-Gly-Phe-Met-NH2 (DALA) and Tyr-d-Ala-d-Ala-Phe-Met-NH2 (TAAFM) all labelled at the methyl group of methionine was studied in the Rhesus monkey. After intravenous administration, the regional kinetics in the head, lungs, liver and …

[Diet planning for hypertensive patients (1800 calories/day). Daily planning for the treatment of hypertension by means of a low sodium, fiber and polyenic acid rich diet].

F Matzkies, G Bieberle-Kling, Mark Baumann, Roland Ernst