Synthesis and N‑Methyl‑d‑aspartate (NMDA) Receptor Activity of Ketamine Metabolites

Synthesis and N‑Methyl‑d‑aspartate (NMDA) Receptor Activity of Ketamine Metabolites

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 hydr...

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Bibliographic Details
Published in:Organic letters Vol. 19; no. 17; pp. 4572 - 4575
Main Authors: Morris, Patrick J, Moaddel, Ruin, Zanos, Panos, Moore, Curtis E, Gould, Todd, Zarate, Carlos A, Thomas, Craig J
Format: Journal Article
Language:English
Published: United States American Chemical Society 01-09-2017
Online Access:Get full text
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Description
Summary: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.
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ORCID
Patrick J. Morris: 0000-0003-2380-4178
ISSN:1523-7060
1523-7052
DOI:10.1021/acs.orglett.7b02177