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Comparison of dihydrodiazepam enantiomers: Metabolism, serum binding and brain receptor binding

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Summary

Dihydrodiazepam is a diazepam prodrug, as shown by its in vitro metabolism by rat and mouse liver and brain microsomal fractions, and its displacing activity on brain diazepam binding. The mechanism of bioactivation is discussed. Stereoselectivity of metabolism and of binding to specific benzodiazepine binding sites in brain synpatosomes and serum albumin were studied.

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Authors and Affiliations

  1. Central Research Institute for Chemistry of the Hungarian Academy of Sciences, Pusztaszeri ut 59, H-1025, Budapest, Hungary

    Zs. Tegyey, G. Maksay, J. Kardos & L. Ötvös

Authors
  1. Zs. Tegyey
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  2. G. Maksay
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  3. J. Kardos
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  4. L. Ötvös
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Additional information

Acknowledgment. The authors are grateful to Dr. J. Wolford for the synthesis of3H-diazepam.

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Tegyey, Z., Maksay, G., Kardos, J. et al. Comparison of dihydrodiazepam enantiomers: Metabolism, serum binding and brain receptor binding. Experientia 36, 1031–1032 (1980). https://doi.org/10.1007/BF01965950

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  • DOI: https://doi.org/10.1007/BF01965950

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