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Differential Inhibition by Cenobamate of Canonical Human Nav1.5 Ion Channels and Several Point Mutants.
Int J Mol Sci
January 2025
Department of Anatomy, Animal Physiology and Biophysics, Faculty of Biology, University of Bucharest, Splaiul Independentei 91-95, 050095 Bucharest, Romania.
Cenobamate is a new and highly effective antiseizure compound used for the treatment of adults with focal onset seizures and particularly for epilepsy resistant to other antiepileptic drugs. It acts on multiple targets, as it is a positive allosteric activator of γ-aminobutyric acid type A (GABA) receptors and an inhibitor of neuronal sodium channels, particularly of the late or persistent Na current. We recently evidenced the inhibitory effects of cenobamate on the peak and late current component of the human cardiac isoform hNav1.
View Article and Find Full Text PDFInhibitory Effects of Cenobamate on Multiple Human Cardiac Ion Channels and Possible Arrhythmogenic Consequences.
Biomolecules
December 2024
Department of Anatomy, Animal Physiology and Biophysics, Faculty of Biology, University of Bucharest, Splaiul Independentei 91-95, 050095 Bucharest, Romania.
Cenobamate is a novel third-generation antiepileptic drug used for the treatment of focal onset seizures and particularly for multi-drug-resistant epilepsy; it acts on multiple targets: GABA receptors (EC 42-194 µM) and persistent neuronal Na currents (IC 59 µM). Side effects include QT interval shortening with >20 ms, but not <300 ms. Our in vitro cardiac safety pharmacology study was performed via whole-cell patch-clamp on HEK293T cells with persistent/inducible expression of human cardiac ion channel isoforms hNav1.
View Article and Find Full Text PDFSea-Island Micelle Structured Hydrogel Scaffold: A Dual-Action Approach to Combat Cartilage Damage under RA Conditions.
ACS Appl Mater Interfaces
January 2025
School of Materials Science and Engineering, University of Science and Technology Beijing, Beijing 100083, China.
Rheumatoid arthritis (RA) is a common autoimmune joint disease characterized by persistent synovial inflammation and cartilage damage. The current clinical treatments primarily utilize drugs such as triptolide (TP) to address inflammation, yet they are unable to directly repair damaged cartilage. Furthermore, the persistent inflammation often undermines the effectiveness of traditional cartilage repair strategies, preventing them from achieving optimal outcomes.
View Article and Find Full Text PDFCenobamate, a New Promising Antiseizure Medication: Experimental and Clinical Aspects.
Int J Mol Sci
December 2024
Department of Pathophysiology, Medical University of Lublin, 20-090 Lublin, Poland.
About 40-50% of patients with drug-resistant epilepsy do not properly respond to pharmacological therapy with antiseizure medications (ASMs). Recently approved by the US Food and Drug Administration and European Medicines Agency as an add-on drug for focal seizures, cenobamate is an ASM sharing two basic mechanisms of action and exhibiting a promising profile of clinical efficacy. The drug preferably inhibits persistent sodium current and activates GABA-mediated events via extrasynaptic, non-benzodiazepine receptors.
View Article and Find Full Text PDFChemical contaminants and environmental stressors induced teratogenic effect in aquatic ecosystem - A comprehensive review.
Toxicol Rep
December 2024
Toxicology and Pharmacology Laboratory, Department of Biotechnology, Faculty of Science and Humanities, SRM Institute of Science and Technology, Kattankulathur, Chengalpattu District, Tamil Nadu 603203, India.
Aquatic environments, including marine and freshwater ecosystems, are vital for ecological balance and biodiversity. The rising global demand for aquaculture products necessitates increased production, with intensified aquaculture practices posing significant environmental risks. This review explores the pathways through which chemical pollutants, heavy metals, pharmaceuticals, and environmental stressors induce teratogenic effects in aquatic species.
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