Summary
MDL 72.974A [(E) 4-fluoro-beta-fluorethylene benzene butanamine] has been shown in animal studies, both in vitro and in vivo, to be a potent, selective, enzyme-activated irreversible inhibitor of MAO-B (Zreika et al., 1989). This compound is under clinical development for the treatment of Parkinson’s disease.
In this double blind, randomized, placebo-controlled normal volunteer study the tolerability, effects on platelet MAO-B activity and associated pharmacokinetics of increasing single oral doses of MDL 72.974A (0.1–12 mg) were assessed.
MDL 72.974A was extremely well tolerated and no treatment-related changes in vital signs or the adjectival check-list (EWL-N) occurred. The compound caused significant dose-dependent inhibition of platelet MAO-B activity at all dose levels with a return to baseline values by day 14. The mean (± S.D.) elimination half-life of parent compound was 51 ± 26 min and mean (± S.D.) urinary excretion was 0.54 ± 0.26% of the administered dose. These results, long action on platelet MAO-B and short elimination half-life, demonstrate MDL 72.974A to be a potent, irreversible inhibitor of MAO-B in man.
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© 1990 Springer-Verlag
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Hinze, C., Harland, D., Zreika, M., Dulery, B., Hardenberg, J. (1990). A double-blind, placebo-controlled study of the tolerability and effects on platelet MAO-B activity of single oral doses of MDL 72.974A in normal volunteers. In: Riederer, P., Youdim, M.B.H. (eds) Amine Oxidases and Their Impact on Neurobiology. Journal of Neural Transmission, vol 32. Springer, Vienna. https://doi.org/10.1007/978-3-7091-9113-2_30
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DOI: https://doi.org/10.1007/978-3-7091-9113-2_30
Publisher Name: Springer, Vienna
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