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


Journal

European archives of psychiatry and clinical neuroscience
ISSN: 1433-8491
Titre abrégé: Eur Arch Psychiatry Clin Neurosci
Pays: Germany
ID NLM: 9103030

Informations de publication

Date de publication:
Oct 2023
Historique:
received: 28 11 2022
accepted: 13 02 2023
medline: 31 8 2023
pubmed: 9 3 2023
entrez: 8 3 2023
Statut: ppublish

Résumé

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.

Identifiants

pubmed: 36890259
doi: 10.1007/s00406-023-01571-4
pii: 10.1007/s00406-023-01571-4
pmc: PMC10465385
doi:

Substances chimiques

Excitatory Amino Acid Antagonists 0
Memantine W8O17SJF3T
Antidepressive Agents 0

Types de publication

Journal Article Review

Langues

eng

Sous-ensembles de citation

IM

Pagination

1463-1476

Informations de copyright

© 2023. The Author(s).

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Auteurs

Maurizio Fava (M)

Department of Psychiatry, Massachusetts General Hospital, Boston, MA, 02114, USA.

Stephen M Stahl (SM)

Department of Psychiatry, VAMC (SD), University of California, San Diego, La Jolla, CA, 92093, USA.
Neuroscience Education Institute, Carlsbad, CA, 92008, USA.

Sara De Martin (S)

Department of Pharmaceutical and Pharmacological Sciences, University of Padua, 35122, Padua, Italy.

Andrea Mattarei (A)

Department of Pharmaceutical and Pharmacological Sciences, University of Padua, 35122, Padua, Italy.

Ezio Bettini (E)

In Vitro Pharmacology Department, Aptuit, an Evotec Company, 37135, Verona, Italy.

Stefano 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.

Andrea 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.

Francesco Bifari (F)

Department of Medical Biotechnology and Translational Medicine, University of Milan, 20122, Milan, Italy.

Luca 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.

Franco Folli (F)

Department of Health Sciences, University of Milan, 20122, Milan, Italy.

Clotilde Guidetti (C)

Child and Adolescent Neuropsychiatry Unit, Department of Neuroscience, Bambino Gesù Pediatric Hospital, 00165, Rome, Italy.

Alberto Furlan (A)

Department of Pharmaceutical and Pharmacological Sciences, University of Padua, 35122, Padua, Italy.

Jacopo Sgrignani (J)

Institute for Research in Biomedicine (IRB), Università della Svizzera Italiana (USI), 6500, Bellinzona, Switzerland.

Patrizia Locatelli (P)

Institute for Research in Biomedicine (IRB), Università della Svizzera Italiana (USI), 6500, Bellinzona, Switzerland.

Andrea Cavalli (A)

Institute for Research in Biomedicine (IRB), Università della Svizzera Italiana (USI), 6500, Bellinzona, Switzerland.
Swiss Institute of Bioinformatics, 1015, Lausanne, Switzerland.

Cedric O'Gorman (C)

Relmada Therapeutics, Coral Gables, FL, 33134, USA.

Sergio Traversa (S)

Relmada Therapeutics, Coral Gables, FL, 33134, USA.

Charles E Inturrisi (CE)

Relmada Therapeutics, Coral Gables, FL, 33134, USA.

Marco Pappagallo (M)

Relmada Therapeutics, Coral Gables, FL, 33134, USA.

Paolo L Manfredi (PL)

Relmada Therapeutics, Coral Gables, FL, 33134, USA. pmanfredi@relmada.com.

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