Synthesis of carbon-14 labeled ketamine and norketamine

被引：7

作者：

Chen, Lu ^{[1
]}

Gong, Yong ^{[1
]}

Salter, Rhys ^{[1
]}

机构：

[1] Johnson & Johnson, Janssen Res & Dev, Isotope Chem & Biotransformat, Spring House, PA 19477 USA

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 2018年 / 61卷 / 11期

关键词：

C-14; labeled; esketamine; ketamine; NMDA receptors; noresketamine; norketamine; synthesis; NMDA-RECEPTOR-ACTIVITY; LABELED KETAMINE; CYCLIC-KETONES; ENANTIOMERS; METABOLITES; AMINATION;

D O I：

10.1002/jlcr.3669

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Ketamine is a well-known general anesthetic that inhibits cerebral NMDA receptors. Norketamine is a major circulating metabolite of this drug. A nasal spray formulation of esketamine, the S enantiomer of ketamine, is under development for the management of treatment-resistant depression. To assess the pharmacokinetic properties, C-14 labeled ketamine and norketamine were prepared separately from commercially available [C-14]CuCN through a five-step sequence with the C-14 label at the quaternary carbon of the cyclohexyl ring. Chiral resolution of [C-14]ketamine and chiral column separation of [C-14]norketamine resolved/separated the (S)-enantiomers from (R)-enantiomers.

引用

页码：864 / 868

页数：5

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