Studies of the biotransformation and pharmacology of ketamine and its metabolites

Leung, Y

Title: Studies of the biotransformation and pharmacology of ketamine and its metabolites

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Abstract

The first part of the research is concerned with the synthesis, resolution and metabolism of norketamine, the primary metabolite of ketamine. Incubations of racemic norketamine, individual enantiomers of norketamine and the pseudoracemates in rat liver microsomes revealed stereoselectivity and enantiomeric interactions during the metabolism of norketamine. The second part of the research describes the synthesis of 6-OH-norketamine, the major secondary metabolite of ketamine, and reports on its pharmacological activity and cerebral distribution in the rat. Primary deuterium isotope effects associated with the metabolism and pharmacological activity of ketamine-N-CD/sub 3/ were examined in the third part of this research. The last part of the research deals with the effect of diazepam on the metabolic transformation of ketamine to norketamine in the rat. The fractions of ketamine metabolized to norketamine were found not to be different in the presence or the absence of diazepam.

Authors:: Leung, Y

Publication Date:: Wed Jan 01 00:00:00 EST 1986

Research Org.:: Washington Univ., Seattle (USA)

OSTI Identifier:: 5349124

Resource Type:: Thesis/Dissertation

Resource Relation:: Other Information: Thesis (Ph. D.)

Country of Publication:: United States

Language:: English

Subject:: 59 BASIC BIOLOGICAL SCIENCES; ANESTHETICS; CHEMICAL PREPARATION; METABOLISM; TRANQUILIZERS; BIOCHEMICAL REACTION KINETICS; BRAIN; DEUTERIUM; ISOTOPE EFFECTS; LIVER; METABOLITES; MICROSOMES; PHARMACOLOGY; RATS; TRACER TECHNIQUES; ANIMALS; BODY; CELL CONSTITUENTS; CENTRAL NERVOUS SYSTEM; CENTRAL NERVOUS SYSTEM AGENTS; CENTRAL NERVOUS SYSTEM DEPRESSANTS; DIGESTIVE SYSTEM; DRUGS; GLANDS; HYDROGEN ISOTOPES; ISOTOPE APPLICATIONS; ISOTOPES; KINETICS; LIGHT NUCLEI; MAMMALS; NERVOUS SYSTEM; NUCLEI; ODD-ODD NUCLEI; ORGANOIDS; ORGANS; PSYCHOTROPIC DRUGS; REACTION KINETICS; RODENTS; STABLE ISOTOPES; SYNTHESIS; VERTEBRATES; 550201* - Biochemistry- Tracer Techniques

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                    Leung, Y. Studies of the biotransformation and pharmacology of ketamine and its metabolites.  United States: N. p., 1986. 
        Web.

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                    Leung, Y. Studies of the biotransformation and pharmacology of ketamine and its metabolites.  United States.

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                    Leung, Y. 1986.  
        "Studies of the biotransformation and pharmacology of ketamine and its metabolites".  United States.

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@article{osti_5349124,

  title        = {Studies of the biotransformation and pharmacology of ketamine and its metabolites},

  author       = {Leung, Y},

  abstractNote = {The first part of the research is concerned with the synthesis, resolution and metabolism of norketamine, the primary metabolite of ketamine. Incubations of racemic norketamine, individual enantiomers of norketamine and the pseudoracemates in rat liver microsomes revealed stereoselectivity and enantiomeric interactions during the metabolism of norketamine. The second part of the research describes the synthesis of 6-OH-norketamine, the major secondary metabolite of ketamine, and reports on its pharmacological activity and cerebral distribution in the rat. Primary deuterium isotope effects associated with the metabolism and pharmacological activity of ketamine-N-CD/sub 3/ were examined in the third part of this research. The last part of the research deals with the effect of diazepam on the metabolic transformation of ketamine to norketamine in the rat. The fractions of ketamine metabolized to norketamine were found not to be different in the presence or the absence of diazepam.},

  doi          = {},

  url          = {https://www.osti.gov/biblio/5349124},
  journal      = {},
number       = ,

  volume       = ,

  place        = {United States},

  year         = {Wed Jan 01 00:00:00 EST 1986},

  month        = {Wed Jan 01 00:00:00 EST 1986}

}

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