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

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Title: Esmethadone-HCl (REL-1017): a promising rapid antidepressant.
Authors: Fava, Maurizio (AUTHOR), Stahl, Stephen M. (AUTHOR), De Martin, Sara (AUTHOR), Mattarei, Andrea (AUTHOR), Bettini, Ezio (AUTHOR), Comai, Stefano (AUTHOR), Alimonti, Andrea (AUTHOR), Bifari, Francesco (AUTHOR), Pani, Luca (AUTHOR), Folli, Franco (AUTHOR), Guidetti, Clotilde (AUTHOR), Furlan, Alberto (AUTHOR), Sgrignani, Jacopo (AUTHOR), Locatelli, Patrizia (AUTHOR), Cavalli, Andrea (AUTHOR), O'Gorman, Cedric (AUTHOR), Traversa, Sergio (AUTHOR), Inturrisi, Charles E. (AUTHOR), Pappagallo, Marco (AUTHOR), Manfredi, Paolo L. (AUTHOR)
Source: European Archives of Psychiatry & Clinical Neuroscience. Oct2023, Vol. 273 Issue 7, p1463-1476. 14p. 2 Diagrams, 6 Charts.
Subjects: Alzheimer's disease, Methyl aspartate receptors, Antidepressants, Neural receptors, Neuroplasticity
Abstract: 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. [ABSTRACT FROM AUTHOR]
Copyright of European Archives of Psychiatry & Clinical Neuroscience is the property of Springer Nature and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract. (Copyright applies to all Abstracts.)
Database: Psychology and Behavioral Sciences Collection
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  Data: Esmethadone-HCl (REL-1017): a promising rapid antidepressant.
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  Data: <searchLink fieldCode="AR" term="%22Fava%2C+Maurizio%22">Fava, Maurizio</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Stahl%2C+Stephen+M%2E%22">Stahl, Stephen M.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22De+Martin%2C+Sara%22">De Martin, Sara</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Mattarei%2C+Andrea%22">Mattarei, Andrea</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Bettini%2C+Ezio%22">Bettini, Ezio</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Comai%2C+Stefano%22">Comai, Stefano</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Alimonti%2C+Andrea%22">Alimonti, Andrea</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Bifari%2C+Francesco%22">Bifari, Francesco</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Pani%2C+Luca%22">Pani, Luca</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Folli%2C+Franco%22">Folli, Franco</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Guidetti%2C+Clotilde%22">Guidetti, Clotilde</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Furlan%2C+Alberto%22">Furlan, Alberto</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Sgrignani%2C+Jacopo%22">Sgrignani, Jacopo</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Locatelli%2C+Patrizia%22">Locatelli, Patrizia</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Cavalli%2C+Andrea%22">Cavalli, Andrea</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22O'Gorman%2C+Cedric%22">O'Gorman, Cedric</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Traversa%2C+Sergio%22">Traversa, Sergio</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Inturrisi%2C+Charles+E%2E%22">Inturrisi, Charles E.</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Pappagallo%2C+Marco%22">Pappagallo, Marco</searchLink> (AUTHOR)<br /><searchLink fieldCode="AR" term="%22Manfredi%2C+Paolo+L%2E%22">Manfredi, Paolo L.</searchLink> (AUTHOR)
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  Data: <searchLink fieldCode="JN" term="%22European+Archives+of+Psychiatry+%26+Clinical+Neuroscience%22">European Archives of Psychiatry & Clinical Neuroscience</searchLink>. Oct2023, Vol. 273 Issue 7, p1463-1476. 14p. 2 Diagrams, 6 Charts.
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  Data: 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. [ABSTRACT FROM AUTHOR]
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  Data: <i>Copyright of European Archives of Psychiatry & Clinical Neuroscience is the property of Springer Nature and its content may not be copied or emailed to multiple sites without the copyright holder's express written permission. Additionally, content may not be used with any artificial intelligence tools or machine learning technologies. However, users may print, download, or email articles for individual use. This abstract may be abridged. No warranty is given about the accuracy of the copy. Users should refer to the original published version of the material for the full abstract.</i> (Copyright applies to all Abstracts.)
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