氯胺酮代谢物的合成及 N-甲基-D-天冬氨酸（NMDA）受体活性。
Synthesis and N-Methyl-d-aspartate (NMDA) Receptor Activity of Ketamine Metabolites.
机构信息
Division of Preclinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health , Rockville, Maryland 20850, United States.
Biomedical Research Center, National Institute on Aging, National Institutes of Health , Baltimore, Maryland 21224, United States.
出版信息
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.
摘要
氯胺酮在人体内迅速代谢为多种代谢物，包括羟基去甲氯胺酮。至少两种羟基去甲氯胺酮在啮齿动物模型中具有显著的抗抑郁作用，对 N-甲基-D-天冬氨酸（NMDA）受体的作用有限。本文介绍了 12 种羟基去甲氯胺酮的合成及其对 NMDA 受体的结合亲和力。
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