Synthesis and N-Methyl-D-aspartate (NMDA) Receptor Activity of Ketamine Metabolites

被引：65

作者：

Morris, Patrick J. ^{[1
]}

Moaddel, Ruin ^{[2
]}

Zanos, Panos ^{[3
]}

Moore, Curtis E. ^{[4
]}

Gould, Todd ^{[3
,5
,6
]}

Zarate, Carlos A., Jr. ^{[7
]}

Thomas, Craig J. ^{[1
]}

机构：

[1] NIH, Div Preclin Innovat, Natl Ctr Adv Translat Sci, Rockville, MD 20850 USA

[2] NIA, Biomed Res Ctr, NIH, Baltimore, MD 21224 USA

[3] Univ Maryland, Sch Med, Dept Psychiat, Baltimore, MD 21201 USA

[4] Univ Calif San Diego, Dept Chem & Biochem, La Jolla, CA 92093 USA

[5] Univ Maryland, Sch Med, Dept Pharmacol, Baltimore, MD 21201 USA

[6] Univ Maryland, Sch Med, Dept Anat & Neurobiol, Baltimore, MD 21201 USA

[7] NIMH, Expt Therapeut & Pathophysiol Branch, NIH, Bethesda, MD 20892 USA

来源：

ORGANIC LETTERS | 2017年 / 19卷 / 17期

关键词：

ANTIDEPRESSANT; MECHANISMS; DEPRESSION; AMINATION; CURRENTS; PLASMA;

D O I：

10.1021/acs.orglett.7b02177

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Ketamine is rapidly metabolized in the human body to a variety of metabolites, including the hydroxynorketamines. At least two hydroxynorketamines have significant antidepressant action in rodent models, with limited action against the N-methyl-D-aspartate (NMDA) receptor. The synthesis of 12 hydroxynorketamines and their binding affinity to the NMDA receptor is presented here.

引用

页码：4572 / 4575

页数：4

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