New Discoveries in the Field of Neuropharmacology

A special issue of Biomolecules (ISSN 2218-273X). This special issue belongs to the section "Molecular Medicine".

Deadline for manuscript submissions: 30 June 2025 | Viewed by 915

Special Issue Editors


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Guest Editor
Department of Anatomy, Animal Physiology and Biophysics, Faculty of Biology, University of Bucharest, 050095 Bucharest, Romania
Interests: blood brain barrier; drug safety; drug arrhythmogenic effects; neuropharmacology; epileptogenesis; depression
Special Issues, Collections and Topics in MDPI journals

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Guest Editor
Department of Anatomy, Animal Physiology and Biophysics, Faculty of Biology, University of Bucharest, 050095 Bucharest, Romania
Interests: biophysical and pharmacological properties of ion channels (particularly ENaC/Deg and TRP channels); mathematical modeling of complex biological systems; applied research in cardiac electrophysiology and cardiac safety drug testing; stem cells – diagnostic and therapeutic applications

Special Issue Information

Dear Colleagues,

This is an inspiring time in biomedical sciences, where new, dynamic methods are being developed and used to produce groundbreaking results in fundamental and applied research, including neuroscience and related fields, such as neuropharmacology. Every year, new promising drugs (new molecular entities) are approved and launched on the market, offering hope to numerous patients affected by severe and debilitating neurologic and psychiatric disorders. This outcome is the result of the systematic application of advanced and highly effective techniques along the different stages of drug R&D pipelines, starting with in silico methods, new in vitro assays, high-throughput screening approaches, animal models of disease, wide genome sequencing and gene expression techniques, powerful transfection vectors, gene editing, stem cells, and many other marvels of modern science. To reflect this extensive progress in neuropharmacology research, we are launching a Special Issue in the prestigious and highly dynamic Biomolecules journal. Therefore, as guest editors, we warmly invite you to contribute by submitting manuscripts containing some of your recent original research results or comprehensive review studies on this topic. We aim to expedite a fair evaluation in this open-access publication of selected papers, offering good scientific visibility.

Yours sincerely,

Dr. Beatrice Mihaela Radu
Dr. Bogdan Amuzescu
Guest Editors

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Keywords

  • neurologic and psychiatric diseases pharmacology
  • in silico drug screening
  • in vitro pharmacology assays
  • animal models
  • neuropharmacogenomics
  • drug safety
  • blood brain barrier
  • electrophysiology
  • patch-clamp

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Published Papers (1 paper)

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Research

19 pages, 6004 KiB  
Article
Inhibitory Effects of Cenobamate on Multiple Human Cardiac Ion Channels and Possible Arrhythmogenic Consequences
by Andreea Larisa Mateias, Florian Armasescu, Bogdan Amuzescu, Alexandru Dan Corlan and Beatrice Mihaela Radu
Biomolecules 2024, 14(12), 1582; https://doi.org/10.3390/biom14121582 - 11 Dec 2024
Viewed by 674
Abstract
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: GABAA receptors (EC50 42–194 µM) and persistent neuronal Na+ currents (IC50 59 µM). Side [...] Read more.
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: GABAA receptors (EC50 42–194 µM) and persistent neuronal Na+ currents (IC50 59 µM). Side effects include QTc 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 hNav1.5 (INa), hCav1.2 (α1c + β2 + α2δ1) (ICaL), hKv7.1 + minK (IKs), and hKv11.1 (hERG) (IKr). We found IC50 of 87.6 µM (peak INa), 46.5 µM (late INa), and 509.75 µM (ICaL). In experiments on Ncyte® ventricular cardiomyocytes, APD90 was reduced with 28.6 ± 13.5% (mean ± SD) by cenobamate 200 µM. Cenobamate’s marked inhibition of INa raises the theoretical possibility of cardiac arrhythmia induction at therapeutic concentrations in the context of preexisting myocardial pathology, in the presence of action potential conduction and repolarization heterogeneity. This hypothetical mechanism is consistent with the known effects of class Ib antiarrhythmics. In simulations with a linear strand of 50 cardiomyocytes with variable inter-myocyte conductance based on a modified O’Hara–Rudy model, we found a negligible cenobamate-induced conduction delay in normal tissue, but a marked delay and also a block when gap junction conduction was already depressed. Full article
(This article belongs to the Special Issue New Discoveries in the Field of Neuropharmacology)
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