A5101915845- Ion channel regulation and function
- Cardiac electrophysiology and arrhythmias
- Neuroscience and Neuropharmacology Research
- Cardiac Arrhythmias and Treatments
- Memory and Neural Mechanisms
- Atrial Fibrillation Management and Outcomes
- Treatment of Major Depression
- Neuroscience and Neural Engineering
- Pharmacological Receptor Mechanisms and Effects
- Receptor Mechanisms and Signaling
- Nicotinic Acetylcholine Receptors Study
- Neonatal Health and Biochemistry
- Peptidase Inhibition and Analysis
- Renal function and acid-base balance
- Signaling Pathways in Disease
- Advanced Memory and Neural Computing
- Botulinum Toxin and Related Neurological Disorders
- Circadian rhythm and melatonin
- Metabolism and Genetic Disorders
- Neurological disorders and treatments
- Neural dynamics and brain function
- Cell Adhesion Molecules Research
United States Military Academy
2004-2017
Bristol-Myers Squibb (United States)
2016-2017
Bristol-Myers Squibb (Germany)
2015
Merck & Co., Inc., Rahway, NJ, USA (United States)
2008
UCB Pharma (Belgium)
2006
University of California, San Diego
2000
Kodolányi János University of Applied Sciences
1982
Novel 3-cyanoisoquinoline Kv1.5 antagonists have been prepared and evaluated in vitro vivo assays for inhibition of the potassium channel its associated cardiac current, IKur. Structural modifications isoquinolinone lead 1 afforded compounds with excellent potency, selectivity, oral bioavailability.
In vitro phenotypic assays of sensory neuron activity are important tools for identifying potential analgesic compounds. These typically characterized by hyperexcitable and/or abnormally, spontaneously active cells. Whereas manual electrophysiology experiments provide high-resolution biophysical data to characterize both in models and therapeutic modalities (e.g., action characteristics, the role specific ion channels, receptors), these techniques hampered their low throughput. We have...
Drug discovery efforts have focused recently on atrial-selective targets, including the Kv1.5 channel, which underlies ultrarapid delayed rectifier current, I<sub>Kur</sub>, to develop novel treatments for atrial fibrillation (AF). Two structurally distinct compounds, a triarylethanolamine TAEA and an isoquinolinone 3-[(dimethylamino)-methyl]-6-methoxy-2-methyl-4-phenylisoquinolin-1(2<i>H</i>)-one (ISQ-1), blocked I<sub>Kur</sub> in Chinese hamster ovary cells expressing human with...