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


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.

SUBMITTER: Morris PJ 

PROVIDER: S-EPMC5641405 | biostudies-literature | 2017 Sep

REPOSITORIES: biostudies-literature

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

Morris Patrick J PJ   Moaddel Ruin R   Zanos Panos P   Moore Curtis E CE   Gould Todd D TD   Zarate Carlos A CA   Thomas Craig J CJ  

Organic letters 20170822 17


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. ...[more]

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