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Chronic TVP-1012 (rasagiline) dose — activity response of monoamine oxidases A and B in the brain of the common marmoset

  • Conference paper
MAO — The Mother of all Amine Oxidases

Part of the book series: Journal of Neural Transmission. Supplement ((NEURAL SUPPL,volume 52))

Summary

The stereospecific form of the known acetylenic mechanismbased MAO-inhibitor AGN1135 (Rasagiline, TVP-1012) is devoid of sympathomimetic amphetamine-like properties.

To evaluate the efficiency and selectivity of subcutaneous injections of TVP-1012 (dose range from 0.01 up to 10mg/kg for 7 days) the activities of monoamine oxidases A and B (MAO-A,-B) were determined in different brain regions of the common marmoset.

At a dose of 0.1mg/kg TVP-1012, almost 80% of MAO-B activity is inhibited in all brain regions investigated (prefrontal and occipital cortex, cerebellum, caudate nucleus, putamen, nucleus accumbens). In contrast, MAO-A is not inhibited in putamen and nucleus accumbens. However, by increasing the TVP-1012 dose to 0.5mg/kg, MAO-A is inhibited to a significant extent as well, concomitant to total inhibition of MAO-B.

The results obtained indicate that TVP-1012 irreversibly inhibits both types of MAO in the common marmoset with selectivity for MAO-B at doses less than 0.5mg/kg. TVP-1012 could be useful in studies requiring selective MAO-B inhibition without concomitant sympathomimetic amphetamine-like effects and could thus be of therapeutic interest for Parkinson’s disease and retarded depression.

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Author information

Authors and Affiliations

  1. Division of Clinical Neurochemistry, Department of Psychiatry, Julius-Maximilians-University, Würzburg, Germany

    Dr. M. E. Götz, W. Breithaupt, P. Riederer & M. Gerlach

  2. Institute of Physiology, Ludwig-Maximilians-University, Munich, Germany

    J. Sautter & A. Kupsch

  3. Department of Neurology / Hospital Grosshadern, Ludwig-Maximilians-University, Munich, Germany

    A. Kupsch, J. Schwarz & W. H. Oertel

  4. Department of Pharmacology, Rappaport Familiy Research Institute, US National Parkinson Foundation, Faculty of Medicine, Technion, Haifa, Israel

    M. B. H. Youdim

  5. Division of Clinical Neurochemistry, University St. Joseph’s Hospital for Neurology, Ruhr-University, Bochum, Germany

    M. Gerlach

  6. Department of Psychiatry, Division of Clinical Neurochemistry, University of Würzburg, Füchsleinstrasse 15, D-97080, Würzburg, Germany

    Dr. M. E. Götz

Authors
  1. Dr. M. E. Götz
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  2. W. Breithaupt
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  3. J. Sautter
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  4. A. Kupsch
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  5. J. Schwarz
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  6. W. H. Oertel
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  7. M. B. H. Youdim
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  8. P. Riederer
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  9. M. Gerlach
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Editor information

Editors and Affiliations

  1. Department of Pharmacology, The Bruce Rappaport Faculty of Medicine, Technion — Israel Institute of Technology, Haifa, Israel

    J. P. M. Finberg  & M. B. H. Youdim  & 

  2. Clinical Neurochemistry, Department of Psychiatry, University of Würzburg, Federal Republic of Germany

    P. Riederer

  3. Biochemistry Department, Trinity College, Dublin, Ireland

    K. F. Tipton

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© 1998 Springer-Verlag Wien

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Götz, M.E. et al. (1998). Chronic TVP-1012 (rasagiline) dose — activity response of monoamine oxidases A and B in the brain of the common marmoset. In: Finberg, J.P.M., Youdim, M.B.H., Riederer, P., Tipton, K.F. (eds) MAO — The Mother of all Amine Oxidases. Journal of Neural Transmission. Supplement, vol 52. Springer, Vienna. https://doi.org/10.1007/978-3-7091-6499-0_27

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  • DOI: https://doi.org/10.1007/978-3-7091-6499-0_27

  • Publisher Name: Springer, Vienna

  • Print ISBN: 978-3-211-83037-6

  • Online ISBN: 978-3-7091-6499-0

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