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Tiplaxtinin, a novel, orally efficacious inhibitor of plasminogen activator inhibitor-1: design, synthesis, and preclinical characterization.
TLDR
The remarkable preclinical safety and metabolic stability profiles of tiplaxtinin led to advancing the compound to clinical trials and in vivo oral efficacy in two different models of acute arterial thrombosis. Expand
Identification of ischemia-regulated phosphorylation sites in connexin43: A possible target for the antiarrhythmic peptide analogue rotigaptide (ZP123).
TLDR
The results suggest that phosphorylation of Ser297 and Ser368 may be involved in functional gating of Cx43 during ischemia and may be possible downstream targets for rotigaptide signaling. Expand
The Antiarrhythmic Peptide Analog ZP123 Prevents Atrial Conduction Slowing During Metabolic Stress
TLDR
This study investigated whether the novel stable antiarrhythmic peptide analog, ZP123, was able to prevent atrial conduction slowing. Expand
Rotigaptide (ZP123) Prevents Spontaneous Ventricular Arrhythmias and Reduces Infarct Size During Myocardial Ischemia/Reperfusion Injury in Open-Chest Dogs
TLDR
It is demonstrated that rotigaptide is a potent antiarrhythmic compound with cardioprotective effects and desirable safety in dogs subjected to a 60-min coronary artery occlusion and 4 h of reperfusion injury. Expand
Discovery of (2S,4R)-1-(2-aminoacetyl)-4-benzamidopyrrolidine-2-carboxylic acid hydrochloride (GAP-134)13, an orally active small molecule gap-junction modifier for the treatment of atrial
TLDR
Small molecule gap-junction modifiers with improved physical properties were identified from a Zealand Pharma peptide library using pharmaceutical profiling, established SAR around 3, and a putative pharmacophore model for rotigaptide. Expand
Effects of Selective Cyclooxygenase-2 Inhibition on Vascular Responses and Thrombosis in Canine Coronary Arteries
TLDR
The results indicate important physiological roles for COX-2–derived prostacyclin and raise concerns regarding an increased risk of acute vascular events in patients receiving COx-2 inhibitors, which may be increased in individuals with underlying inflammatory disorders. Expand
The Antiarrhythmic Peptide Rotigaptide (ZP123) Increases Connexin 43 Protein Expression in Neonatal Rat Ventricular Cardiomyocytes
TLDR
The findings suggest that rotigaptide's effect on Cx43 expression is partly due to increased biosynthesis, and it is suggested that this peptide is a novel antiarrhythmic peptide applicable to protein synthesis. Expand
Effects of Chronic Gap Junction Conduction–Enhancing Antiarrhythmic Peptide GAP-134 Administration on Experimental Atrial Fibrillation in Dogs
TLDR
Oral GAP-134 reduces pacing-induced decrease in LA wavelength and appears to attenuate AF vulnerability in dogs with less atrial mechanical remodeling, and Gap junction modulation may affect AF in some circumstances. Expand
Pharmacological modulation of gap junction function with the novel compound rotigaptide: a promising new principle for prevention of arrhythmias.
TLDR
Rotigaptide represents a pioneering pharmacological principle with a highly favourable preclinical and clinical safety profile, which makes this molecule a promising drug candidate for the prevention of cardiac arrhythmias. Expand
Treatment With the Gap Junction Modifier Rotigaptide (ZP123) Reduces Infarct Size in Rats With Chronic Myocardial Infarction
TLDR
It is concluded that whereas treatment with non-selective inhibitors of gap junction intercellular communication cause a reduction in infarct size, this information cannot be extrapolated to the effects of compounds that selectively increase gap junction Intercellular Communication. Expand
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