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

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

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.

Publication types

  • Research Support, N.I.H., Intramural

MeSH terms

  • Antidepressive Agents
  • Ketamine / metabolism*
  • Molecular Structure
  • N-Methylaspartate
  • Receptors, N-Methyl-D-Aspartate

Substances

  • Antidepressive Agents
  • Receptors, N-Methyl-D-Aspartate
  • N-Methylaspartate
  • Ketamine