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[3H]-Norcocaine and [3H]-pseudococaine: Effect of N-demethylation and C2-epimerization of cocaine on its pharmacokinetics in the rat

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Summary

After i.v. injections of cocaine, norcocaine, pseudococaine to the rat, the T1/2 in brain were 0.4, 0.6, 0.2 h respectively and in plasma 0.4, 0.5, 0.2 h respectively. Benzoylnorecgonine and norecgonine were the metabolites of norcocaine in brain. Pseudonorcocaine, pseudobenzoylnorecgonine, pseudobenzoylecgonine and pseudoecgonine were the metabolites of pseudococaine in rat brain. Benzoylnorecgonine and pseudobenzoylecgonine had potent stimulant activity intracisternally in the rats.

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Authors and Affiliations

  1. Testing and Research Laboratory, New York State Office of Drug Abuse Services, 80 Hanson Place, 11217, Brooklyn, New York, USA

    A. L. Misra, R. B. Pontani & S. J. Mule'

Authors
  1. A. L. Misra
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  2. R. B. Pontani
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  3. S. J. Mule'
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Additional information

Acknowledgment. This work was supported by U.S. Army Medical Research and Development Command Contract No. DADA-17-73-C-3080.

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Misra, A.L., Pontani, R.B. & Mule', S.J. [3H]-Norcocaine and [3H]-pseudococaine: Effect of N-demethylation and C2-epimerization of cocaine on its pharmacokinetics in the rat. Experientia 32, 895–897 (1976). https://doi.org/10.1007/BF02003753

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  • DOI: https://doi.org/10.1007/BF02003753

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