Advertisement

Effects of the COMT inhibitor, CGP 28014, on plasma homovanillic acid and O-methylation of exogenous L-DOPA in the rat

  • P. C. Waldmeier
  • P. De Herdt
  • L. Maitre
Conference paper
Part of the Journal of Neural Transmission book series (NEURAL SUPPL, volume 32)

Summary

Methods potentially suitable for the determination of the COMT inhibitory properties of CGP 28014 (N-(2-pyridone-6-yl)-N′,N′-di-n-propylformamidine) in humans were tested in rats: the measurement of effects on HVA levels and on the conversion of exogenously administered L-DOPA into its O-methylated derivative, in serum and striatum. The compound decreased HVA as well as the conversion of L-DOPA to O-methyl-DOPA similarly in serum and striatum. The latter parameter was considered to be more useful for the assessment of COMT inhibition in humans, because it is less affected by diurnal changes, dietary effects, physical activity etc.

Keywords

Vanillic Acid COMT Inhibitor Trunk Blood Aromatic Amino Acid Decarboxylase Coulometric Detection 
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.

Preview

Unable to display preview. Download preview PDF.

Unable to display preview. Download preview PDF.

References

  1. Männistö PT, Kaakkola S (1989) New selective COMT inhibitors: useful adjuncts for Parkinson’s disease?. TIPS 10:54–56.PubMedGoogle Scholar
  2. Sternberg DE, Heninger GR, Roth RH (1983) Plasma homovanillic acid as an index of brain dopamine metabolism: enhancement with debrisoquin. Life Sci 32:2447–2452.PubMedCrossRefGoogle Scholar
  3. Waldmeier PC, Feldtrauer JJ (1987) On the role of O-methylation in the metabolism of S-adenosylmethionine in rat brain. Biochem Pharmacol 36:2855–2861.PubMedCrossRefGoogle Scholar
  4. Waldmeier PC, Feldtrauer JJ, Hauser K, Bittiger H, Bischoff S, von Sprecher G (1990) CGP 28014, a new non-catecholic COMT inhibitor. Naunyn Schmiedebergs Arch Pharmacol 341 [Suppl] R 97 (abstract no 386).Google Scholar

Copyright information

© Springer-Verlag 1990

Authors and Affiliations

  • P. C. Waldmeier
    • 1
  • P. De Herdt
    • 1
  • L. Maitre
    • 1
  1. 1.Research Department, Pharmaceuticals DivisionCiba-Geigy Ltd.BaselSwitzerland

Personalised recommendations