Pharmacological Insight into NMDA Receptor Antagonists

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: 15 July 2024 | Viewed by 1524

Special Issue Editor


E-Mail Website
Guest Editor
Institut de Pharmacologie et de Biologie Structurale, Université de Toulouse, CNRS, UPS, 31059 Toulouse, France
Interests: NMDA receptor; G-protein-coupled receptors; opioid receptors; antidepressants; neurological disorders; multiple sclerosis

Special Issue Information

Dear Colleagues,

The N-methyl-D-aspartate (NMDA) receptor belongs to the glutamate sensing receptor family. This ionotropic hetero-tetrameric receptor displays an essential neuronal function and is deeply implicated in memory and learning processes, and is more consistently associated with synaptic plasticity in the central nervous system. The activation of NMDA receptors follows the binding of two co-agonists amino acids, glutamate and glycine, as well as the removal of blocking Mg2+ ions from the inner channel via membrane depolarization and Ca++ entry in neuron dendrites. Besides the physiological role of NMDA receptors, this receptor is also known for inferring the hallucinogenic effects of recreational drugs (such as ketamine, PCP, or dextromethorphan). Research on new drug candidates acting as noncompetitive NMDA antagonists has had renewed interest since ketamine (esketamine) has been repurposed as an antidepressant. The search for new radiotracers that can discriminate the open state of the NMDA receptor in the context of neurodegenerative diseases is also of major importance.

In this Special Issue, we aim to draw together research from experts in a field that highlights new drugs and radiotracers that act as noncompetitive NMDA antagonists.

I look forward to your valuable contribution.

Dr. Franck Jean Talmont
Guest 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. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). 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

  • ionotropic receptors
  • NMDA receptors
  • antidepressants
  • radiotracers
  • neurodegenerative diseases

Published Papers (1 paper)

Order results
Result details
Select all
Export citation of selected articles as:

Research

19 pages, 2031 KiB  
Article
Use of Quantitative Electroencephalography to Inform Age- and Sex-Related Differences in NMDA Receptor Function Following MK-801 Administration
by Kimberly M. Holter, Alex D. Lekander, Bethany E. Pierce, L. Paul Sands and Robert W. Gould
Pharmaceuticals 2024, 17(2), 237; https://doi.org/10.3390/ph17020237 - 11 Feb 2024
Viewed by 1038
Abstract
Sex- and age-related differences in symptom prevalence and severity have been widely reported in patients with schizophrenia, yet the underlying mechanisms contributing to these differences are not well understood. N-methyl-D-aspartate (NMDA) receptor hypofunction contributes to schizophrenia pathology, and preclinical models often use [...] Read more.
Sex- and age-related differences in symptom prevalence and severity have been widely reported in patients with schizophrenia, yet the underlying mechanisms contributing to these differences are not well understood. N-methyl-D-aspartate (NMDA) receptor hypofunction contributes to schizophrenia pathology, and preclinical models often use NMDA receptor antagonists, including MK-801, to model all symptom clusters. Quantitative electroencephalography (qEEG) represents a translational approach to measure neuronal activity, identify targetable biomarkers in neuropsychiatric disorders and evaluate possible treatments. Abnormalities in gamma power have been reported in patients with schizophrenia and correspond to psychosis and cognitive impairment. Further, as gamma power reflects cortical glutamate and GABA signaling, it is highly sensitive to changes in NMDA receptor function, and NMDA receptor antagonists aberrantly increase gamma power in rodents and humans. To evaluate the role of sex and age on NMDA receptor function, MK-801 (0.03–0.3 mg/kg, SC) was administered to 3- and 9-month-old male and female Sprague–Dawley rats that were implanted with wireless EEG transmitters to measure cortical brain function. MK-801-induced elevations in gamma power were observed in 3-month-old male and female and 9-month-old male rats. In contrast, 9-month-old female rats demonstrated blunted maximal elevations across a wide dose range. Importantly, MK-801-induced hyperlocomotor effects, a common behavioral screen used to examine antipsychotic-like activity, were similar across all groups. Overall, sex-by-age-related differences in gamma power support using qEEG as a translational tool to evaluate pathological progression and predict treatment response across a heterogeneous population. Full article
(This article belongs to the Special Issue Pharmacological Insight into NMDA Receptor Antagonists)
Show Figures

Figure 1

Back to TopTop