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MDPIMDPI

3 Results Found

  • Perspective
  • Open Access
20 Citations
4,129 Views
12 Pages
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Esmethadone (REL-1017) and Other Uncompetitive NMDAR Channel Blockers May Improve Mood Disorders via Modulation of Synaptic Kinase-Mediated Signaling

  • Stephen M. Stahl,
  • Sara De Martin,
  • Andrea Mattarei,
  • Ezio Bettini,
  • Luca Pani,
  • Clotilde Guidetti,
  • Franco Folli,
  • Marc de Somer,
  • Sergio Traversa and
  • Paolo L. Manfredi
  • + 5 authors
Int. J. Mol. Sci.2022, 23(20), 12196;https://doi.org/10.3390/ijms232012196

13 October 2022

This article presents a mechanism of action hypothesis to explain the rapid antidepressant effects of esmethadone (REL-1017) and other uncompetitive N-methyl-D-aspartate receptor (NMDAR) antagonists and presents a corresponding mechanism of disease h...

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  • Article
  • Open Access
13 Citations
4,389 Views
17 Pages
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The N-Methyl-D-Aspartate Receptor Blocker REL-1017 (Esmethadone) Reduces Calcium Influx Induced by Glutamate, Quinolinic Acid, and Gentamicin

  • Ezio Bettini,
  • Sara De Martin,
  • Andrea Mattarei,
  • Marco Pappagallo,
  • Stephen M. Stahl,
  • Francesco Bifari,
  • Charles E. Inturrisi,
  • Franco Folli,
  • Sergio Traversa and
  • Paolo L. Manfredi
Pharmaceuticals2022, 15(7), 882;https://doi.org/10.3390/ph15070882

17 July 2022

REL-1017 (esmethadone) is a novel N-methyl-D-aspartate receptor (NMDAR) antagonist and promising rapid antidepressant candidate. Using fluorometric imaging plate reader (FLIPR) assays, we studied the effects of quinolinic acid (QA) and gentamicin, wi...

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  • Article
  • Open Access
27 Citations
4,844 Views
22 Pages
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Pharmacological Comparative Characterization of REL-1017 (Esmethadone-HCl) and Other NMDAR Channel Blockers in Human Heterodimeric N-Methyl-D-Aspartate Receptors

  • Ezio Bettini,
  • Stephen M. Stahl,
  • Sara De Martin,
  • Andrea Mattarei,
  • Jacopo Sgrignani,
  • Corrado Carignani,
  • Selena Nola,
  • Patrizia Locatelli,
  • Marco Pappagallo and
  • Paolo L. Manfredi
  • + 8 authors
Pharmaceuticals2022, 15(8), 997;https://doi.org/10.3390/ph15080997

13 August 2022

Excessive Ca2+ currents via N-methyl-D-aspartate receptors (NMDARs) have been implicated in many disorders. Uncompetitive NMDAR channel blockers are an emerging class of drugs in clinical use for major depressive disorder (MDD) and other neuropsychia...

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