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State-of-the-Art Molecular Pharmacology in Netherlands
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State-of-the-Art Molecular Pharmacology in Netherlands

A special issue of International Journal of Molecular Sciences (ISSN 1422-0067). This special issue belongs to the section "Molecular Pharmacology".

Deadline for manuscript submissions: closed (31 October 2022) | Viewed by 2716

Special Issue Editor

Prof. Dr. Godefridus J. (Frits) Peters

E-Mail Website
Collection Editor
1. Department of Medical Oncology, Cancer Center Amsterdam, Amsterdam UMC, VU University Medical Center (VUmc), De Boelelaan 1117, 1081 HV Amsterdam, The Netherlands
2. Department of Biochemistry, Medical University of Gdansk, 80-210 Gdansk, Poland
Interests: cancer
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Pharmacology is a discipline that deals with the interactions between natural, semisynthetic, or fully (bio)synthetic therapeutic agents at the cellular and organismal levels. These therapeutic agents can be small molecules or macromolecules, such as proteins and antibodies. Thus, this subject is positioned at the interface of pharmacy/chemistry and physiology/pathophysiology in their broadest senses. It operates at various organizational levels, such as the molecular, subcellular, cellular, organ, and systemic platforms. Molecular pharmacology investigates the molecular mode of action of therapeutic agents using cellular, genetic, and molecular biology approaches, and is among the most rapidly developing fields of pharmacology.

Original research and review articles on molecular pharmacology are invited. The “Molecular Pharmacology” section aims to publish the latest developments in cellular and molecular pharmacology with a major emphasis on the mechanism of action of novel drugs, innovative pharmacological technologies, cell signaling, transduction pathway analysis, genomics, proteomics, and metabonomics applications to study drug action. An additional focus will be the way in which normal biological function is illuminated by knowledge of the action of drugs at the cellular and molecular levels.

A great number of research teams in the Netherlands from different institutions and universities are working together and devoting considerable effort to developing and studying molecular pharmacology. This Topical Collection is committed to providing an overview of the macromolecular sciences and technologies in the Netherlands.

Prof. Dr. Godefridus J. (Frits) Peters
Collection Editor

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. International Journal of Molecular Sciences is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. There is an Article Processing Charge (APC) for publication in this open access journal. For details about the APC please see here. Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

  • signal transduction
  • receptor
  • animal models
  • preclinical
  • pharmacodynamics
  • pharmacokinetics
  • drug development
  • drug metabolism

Published Papers (1 paper)

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Research

19 pages, 2353 KiB  
Article
The Antidepressant Paroxetine Reduces the Cardiac Sodium Current
by Ingmar S. Plijter, Arie O. Verkerk and Ronald Wilders
Int. J. Mol. Sci. 2023, 24(3), 1904; https://doi.org/10.3390/ijms24031904 - 18 Jan 2023
Cited by 2 | Viewed by 2235
Abstract
A considerable amount of literature has been published on antidepressants and cardiac ion channel dysfunction. The antidepressant paroxetine has been associated with Brugada syndrome and long QT syndrome, albeit on the basis of conflicting findings. The cardiac voltage-gated sodium channel (NaV1.5) [...] Read more.
A considerable amount of literature has been published on antidepressants and cardiac ion channel dysfunction. The antidepressant paroxetine has been associated with Brugada syndrome and long QT syndrome, albeit on the basis of conflicting findings. The cardiac voltage-gated sodium channel (NaV1.5) is related to both of these syndromes, suggesting that paroxetine may have an effect on this channel. In the present study, we therefore carried out patch clamp experiments to examine the effect of paroxetine on human NaV1.5 channels stably expressed in human embryonic kidney 293 (HEK-293) cells as well as on action potentials of isolated rabbit left ventricular cardiomyocytes. Additionally, computer simulations were conducted to test the functional effects of the experimentally observed paroxetine-induced changes in the NaV1.5 current. We found that paroxetine led to a decrease in peak NaV1.5 current in a concentration-dependent manner with an IC50 of 6.8 ± 1.1 µM. In addition, paroxetine caused a significant hyperpolarizing shift in the steady-state inactivation of the NaV1.5 current as well as a significant increase in its rate of inactivation. Paroxetine (3 µM) affected the action potential of the left ventricular cardiomyocytes, significantly decreasing its maximum upstroke velocity and amplitude, both of which are mainly regulated by the NaV1.5 current. Our computer simulations demonstrated that paroxetine substantially reduces the fast sodium current of human left ventricular cardiomyocytes, thereby slowing conduction and reducing excitability in strands of cells, in particular if conduction and excitability are already inhibited by a loss-of-function mutation in the NaV1.5 encoding SCN5A gene. In conclusion, paroxetine acts as an inhibitor of NaV1.5 channels, which may enhance the effects of loss-of-function mutations in SCN5A. Full article
(This article belongs to the Special Issue State-of-the-Art Molecular Pharmacology in Netherlands)
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