• Publications
  • Influence
The Two Mechanisms of Action of Racemic Cardiotonic EMD 53998, Calcium Sensitization and Phosphodiesterase Inhibition, Reside in Different Enantiomers
The novel cardiotonic EMD 53 998 increases contractile force in vitro through both inhibition of phosphodiesterase III (PDE III) activity and increase in the responsiveness of the contractileExpand
Novel diazinone derivatives separate myofilament Ca2+ sensitization and phosphodiesterase III inhibitory effects in guinea pig myocardium.
The inotropic state of the myocardium can be enhanced via an increase in cell Ca2+ loading or in myofilament responsiveness to Ca2+. Although different pharmacological agents combine theseExpand
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.
OBJECTIVE The aim was to assess whether bimakalim, an opener of ATP sensitive potassium channels, can reduce infarct size in swine myocardium. METHODS Experiments were performed in open chest pigsExpand
Calcium Sensitization as a Positive Inotropic Mechanism in Diseased Rat and Human Heart
The two isomers of the positive inotropic compound EMD 53998, (+)EMD 57033 and (-)EMD 57439, possess selective calcium sensitizing and phosphodiesterase (PDE) inhibitory properties, respectively. WeExpand
A phase 1 study to evaluate the safety and pharmacokinetics of PQ912, a glutaminyl cyclase inhibitor, in healthy subjects
Pyroglutamate‐amyloid‐β (pE‐Aβ) peptides are major components of Aβ‐oligomers and Aβ‐plaques, which are regarded as key culprits of Alzheimer's disease (AD) pathology. PQ912 is a competitiveExpand
Central and peripheral actions of the novel κ‐opioid receptor agonist, EMD 60400
1 The pharmacological characteristics of the κ‐opioid receptor agonist, EMD 60400, have been investigated, with particular reference to its central and peripheral sites of action and its ability toExpand
Involvement of ATP-sensitive potassium channels in preconditioning protection
SummarySingle or multiple brief periods of ischemia (preconditioning, PC) have been shown to protect the myocardium from infarction during a subsequent more prolonged ischemic insult. To test theExpand
Passive Aβ Immunotherapy: Current Achievements and Future Perspectives
Passive immunotherapy has emerged as a very promising approach for the treatment of Alzheimer’s disease and other neurodegenerative disorders, which are characterized by the misfolding and depositionExpand
Safety, tolerability and efficacy of the glutaminyl cyclase inhibitor PQ912 in Alzheimer’s disease: results of a randomized, double-blind, placebo-controlled phase 2a study
BackgroundPQ912 is an inhibitor of the glutaminyl cyclase enzyme that plays a central role in the formation of synaptotoxic pyroglutamate-A-beta oligomers. We report on the first clinical study withExpand
EMD 53998 acts as Ca2+-sensitizer and phosphodiesterase III-inhibitor in human myocardium
The effect of EMD 53998 (EMD) (0.1–100 μmol/l), chemically a racemic thiadiazinone derivative, suggested to be a potent Ca2+-sensitizer, was studied in human failing and nonfailing left ventricularExpand