Esmethadone-HCl (REL-1017): a promising rapid antidepressant.

Autor: Fava M; Department of Psychiatry, Massachusetts General Hospital, Boston, MA, 02114, USA., Stahl SM; Department of Psychiatry, VAMC (SD), University of California, San Diego, La Jolla, CA, 92093, USA.; Neuroscience Education Institute, Carlsbad, CA, 92008, USA., De Martin S; Department of Pharmaceutical and Pharmacological Sciences, University of Padua, 35122, Padua, Italy., Mattarei A; Department of Pharmaceutical and Pharmacological Sciences, University of Padua, 35122, Padua, Italy., Bettini E; In Vitro Pharmacology Department, Aptuit, an Evotec Company, 37135, Verona, Italy., Comai S; Department of Pharmaceutical and Pharmacological Sciences, University of Padua, 35122, Padua, Italy.; Department of Biomedical Sciences, University of Padua, 35122, Padua, Italy.; Department of Psychiatry, McGill University, Montreal, QC, H3A 1A1, Canada., Alimonti A; Department of Health Sciences and Technology, ETH Zurich, 8092, Zurich, Switzerland.; Institute of Oncology Research (IOR), Oncology Institute of Southern Switzerland (IOSI), 6500, Bellinzona, Switzerland.; Università della Svizzera Italiana, 6900, Lugano, Switzerland.; Veneto Institute of Molecular Medicine, 35129, Padua, Italy.; Department of Medicine-DIMED, University of Padua, 35122, Padua, Italy., Bifari F; Department of Medical Biotechnology and Translational Medicine, University of Milan, 20122, Milan, Italy., Pani L; Relmada Therapeutics, Coral Gables, FL, 33134, USA.; Department of Psychiatry and Behavioral Sciences, School of Medicine, University of Miami, Miami, FL, 33146, USA.; Department of Biomedical, Metabolic and Neural Sciences, University of Modena and Reggio Emilia, 41121, Modena, Italy., Folli F; Department of Health Sciences, University of Milan, 20122, Milan, Italy., Guidetti C; Child and Adolescent Neuropsychiatry Unit, Department of Neuroscience, Bambino Gesù Pediatric Hospital, 00165, Rome, Italy., Furlan A; Department of Pharmaceutical and Pharmacological Sciences, University of Padua, 35122, Padua, Italy., Sgrignani J; Institute for Research in Biomedicine (IRB), Università della Svizzera Italiana (USI), 6500, Bellinzona, Switzerland., Locatelli P; Institute for Research in Biomedicine (IRB), Università della Svizzera Italiana (USI), 6500, Bellinzona, Switzerland., Cavalli A; Institute for Research in Biomedicine (IRB), Università della Svizzera Italiana (USI), 6500, Bellinzona, Switzerland.; Swiss Institute of Bioinformatics, 1015, Lausanne, Switzerland., O'Gorman C; Relmada Therapeutics, Coral Gables, FL, 33134, USA., Traversa S; Relmada Therapeutics, Coral Gables, FL, 33134, USA., Inturrisi CE; Relmada Therapeutics, Coral Gables, FL, 33134, USA., Pappagallo M; Relmada Therapeutics, Coral Gables, FL, 33134, USA., Manfredi PL; Relmada Therapeutics, Coral Gables, FL, 33134, USA. pmanfredi@relmada.com.
Jazyk: angličtina
Zdroj: European archives of psychiatry and clinical neuroscience [Eur Arch Psychiatry Clin Neurosci] 2023 Oct; Vol. 273 (7), pp. 1463-1476. Date of Electronic Publication: 2023 Mar 08.
DOI: 10.1007/s00406-023-01571-4
Abstrakt: This review article presents select recent studies that form the basis for the development of esmethadone into a potential new drug. Esmethadone is a promising member of the pharmacological class of uncompetitive N-methyl-D-aspartate receptor (NMDAR) antagonists that have shown efficacy for major depressive disorder (MDD) and other diseases and disorders, such as Alzheimer's dementia and pseudobulbar affect. The other drugs in the novel class of NMDAR antagonists with therapeutic uses that are discussed for comparative purposes in this review are esketamine, ketamine, dextromethorphan, and memantine. We present in silico, in vitro, in vivo, and clinical data for esmethadone and other uncompetitive NMDAR antagonists that may advance our understanding of the role of these receptors in neural plasticity in health and disease. The efficacy of NMDAR antagonists as rapid antidepressants may advance our understanding of the neurobiology of MDD and other neuropsychiatric diseases and disorders.
(© 2023. The Author(s).)
Databáze: MEDLINE
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