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Ring-substituted analogues of tranylcypromine as monoamine oxidase inhibitors

  • R. L. Sherry
  • G. B. Baker
  • R. T. Coutts
  • D. D. Mousseau
Conference paper
Part of the Journal of Neural Transmission book series (NEURAL SUPPL, volume 32)

Summary

4-Fluorotranylcypromine and 4-methoxytranylcypromine, in which the 4-position of the phenyl ring is protected from metabolic ring hydroxylation, were tested for their ability to inhibit, relative to tranylcypromine, monoamine oxidase (MAO) -A and -B in rat brain after administration of low doses (1.2 and 3.7 μmol/kg) of the drugs. One hour after intraperitoneal injection of the lower dose, tranylcypromine was weaker than 4-fluorotranylcypromine and 4-methoxytranylcypromine at inhibiting MAO-A. After long-term (28 day) administration of a dose of 3.7 μmol/kg/day (administered via osmotic minipumps), 4-fluorotranylcypromine had a slightly stronger inhibitory effect on MAO-B than did the other two drugs. At the same time and dose both 4-substituted analogues were slightly more potent inhibitors of MAO-A than was tranylcypromine. After 28 days of administration at a daily dose of 1.2 μmol/kg/day, both analogues produced greater inhibition of MAO-A and -B than did tranylcypromine. 4-Methoxytranylcypromine and 4-fluorotranylcypromine were similar in their extent of inhibition of MAO-B but the former was more potent than the latter at inhibition MAO-A.

Keywords

Monoamine Oxidase Monoamine Oxidase Inhibitor Osmotic Minipumps BioI Psychiatry Neurotransmitter Amine 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Springer-Verlag 1990

Authors and Affiliations

  • R. L. Sherry
    • 1
  • G. B. Baker
    • 1
  • R. T. Coutts
    • 1
  • D. D. Mousseau
    • 1
  1. 1.Neurochemical Research Unit and PMHAC Research Unit, Department of PsychiatryUniversity of AlbertaEdmontonCanada

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