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Org Lett. 2017 Sep 1;19(17):4572-4575. doi: 10.1021/acs.orglett.7b02177. Epub 2017 Aug 22.

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

Author information

1
Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health , Rockville, Maryland 20850, United States.
2
Biomedical Research Center, National Institute on Aging, National Institutes of Health , Baltimore, Maryland 21224, United States.
3
Department of Psychiatry, University of Maryland School of Medicine , Baltimore, Maryland 21201, United States.
4
Department of Chemistry and Biochemistry, University of California, San Diego , La Jolla, California 92093, United States.
5
Departments of Psychiatry, Pharmacology, and Anatomy & Neurobiology, University of Maryland School of Medicine , Baltimore, Maryland 21201, United States.
6
Experimental Therapeutics and Pathophysiology Branch, National Institute of Mental Health, National Institutes of Health , Bethesda, Maryland 20892, United States.

Abstract

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.

PMID:
28829612
PMCID:
PMC5641405
DOI:
10.1021/acs.orglett.7b02177
[Indexed for MEDLINE]
Free PMC Article

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