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The Two Mechanisms of Action of Racemic Cardiotonic EMD 53998, Calcium Sensitization and Phosphodiesterase Inhibition, Reside in Different Enantiomers
TLDR
It is concluded that one of the two different mechanisms underlying the overall positive inotropic activity of EMD 53 998 can be assigned, almost exclusively, to one ofThe two enantiomer EMD 57 033 is unique in possessing both a high absolute potency at the level of the contractile elements and a favorable relation of Ca2+ sensitization to PDE inhibition.
Novel diazinone derivatives separate myofilament Ca2+ sensitization and phosphodiesterase III inhibitory effects in guinea pig myocardium.
TLDR
Investigation of the effects and mechanism of action of novel diazinone derivatives on guinea pig myocardial preparations indicates that structural changes in the d Diazinone molecule shift the mechanism ofaction for the positive inotropic effect of the diazInone derivatives in the intact cell from a predominant myofilament sensitization to an enhancement in cell Ca2+ loading and an augmentation in the Cai transient (EMD 54650).
Effect of bimakalim (EMD 52692), an opener of ATP sensitive potassium channels, on infarct size, coronary blood flow, regional wall function, and oxygen consumption in swine.
TLDR
The data are consistent with the hypothesis that bimakalim reduces infarct size by activation of cardiac ATP sensitive potassium channels and not through unloading of the heart because of its vasodilator effects.
Calcium Sensitization as a Positive Inotropic Mechanism in Diseased Rat and Human Heart
TLDR
The limited inotropic response in severely failing human myocardium, together with possible vasorelaxation, may provide cardiac support in heart failure without an excessive increase in cardiac O2 demand.
Involvement of ATP-sensitive potassium channels in preconditioning protection
TLDR
It is concluded that in swine myocardium KATP channels are involved in the protective effect of ischemic preconditioning, since glibenclamide completely abolished the Protective effect of preconditionsing, while bimakalim could — at least in part — mimic it.
Passive Aβ Immunotherapy: Current Achievements and Future Perspectives
TLDR
A special focus is placed on molecules that are directed against post-translationally modified variants of the Aβ peptide, an emerging approach for development of new antibody molecules.
Central and peripheral actions of the novel κ‐opioid receptor agonist, EMD 60400
TLDR
The action of EMD 60400 in the hyperalgesic pressure pain test was completely antagonized by injection of the κ‐opioid antagonist, norbinaltorphimine (100 μg) into the inflamed tissue, thus demonstrating the peripheral opioid nature of this effect.
EMD 53998 acts as Ca2+-sensitizer and phosphodiesterase III-inhibitor in human myocardium
TLDR
EMD is a potent calcium sensitizing agent in human myocardium via sensitizing of the contractile proteins towards Ca2+ and by inhibition of phosphodiesterase III-isoenzymes and could be one step in the evolution to more potent and selective calcium-sensitizers.
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