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依他佐辛盐酸盐(REL-1017):一种有前途的快速抗抑郁药。

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

机构信息

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

Department of Psychiatry, VAMC (SD), University of California, San Diego, La Jolla, CA, 92093, USA.

出版信息

Eur Arch Psychiatry Clin Neurosci. 2023 Oct;273(7):1463-1476. doi: 10.1007/s00406-023-01571-4. Epub 2023 Mar 8.

DOI:10.1007/s00406-023-01571-4
PMID:36890259
原文链接:
https://pmc.ncbi.nlm.nih.gov/articles/PMC10465385/
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.

摘要

这篇综述文章介绍了一些最近的研究,这些研究为埃索美拉唑酮的开发奠定了基础,埃索美拉唑酮可能成为一种新的药物。埃索美拉唑酮是一种很有前途的非竞争性 N-甲基-D-天冬氨酸受体 (NMDAR) 拮抗剂药物,已被证明对重度抑郁症 (MDD) 和其他疾病和障碍有效,如阿尔茨海默病痴呆和假性延髓情绪。在本综述中,为了进行比较,还讨论了具有治疗用途的新型 NMDAR 拮抗剂类别的其他药物,包括埃司他美酮、氯胺酮、右美沙芬和美金刚。我们介绍了埃索美拉唑酮和其他非竞争性 NMDAR 拮抗剂的计算、体外、体内和临床数据,这些数据可能有助于我们了解这些受体在健康和疾病中的神经可塑性中的作用。NMDAR 拮抗剂作为快速抗抑郁药的疗效可能有助于我们理解 MDD 和其他神经精神疾病的神经生物学。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e0d/10465385/e8b7a75d7247/406_2023_1571_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e0d/10465385/7534fdab1be2/406_2023_1571_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e0d/10465385/e8b7a75d7247/406_2023_1571_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e0d/10465385/7534fdab1be2/406_2023_1571_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6e0d/10465385/e8b7a75d7247/406_2023_1571_Fig2_HTML.jpg

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3
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