The antiparkinsonian agent budipine is an N-methyl-D-aspartate antagonist

  • T. Klockgether
  • P. Jacobsen
  • P. -A. Löschmann
  • L. Turski
Full Papers

DOI: 10.1007/BF02251200

Cite this article as:
Klockgether, T., Jacobsen, P., Löschmann, P.A. et al. J Neural Transm Gen Sect (1993) 5: 101. doi:10.1007/BF02251200

Summary

Budipine (1-t-butyl-4,4-diphenylpiperidine) is a novel antiparkinsonian agent. Its clinical efficacy has been proven in double-blind placebo-controlled trials. The mechanism of action of budipine, however, is unknown. Budipine selectively increased the threshold of N-methyl-D-aspartate (NMDA)-induced seizures in mice. Similar to known specific NMDA antagonist, budipine depressed polysynaptic spinal reflexes in mice, but had no consistent effect on spinal monosynaptic reflexes. In receptor binding experiments, budipine displaced thienylcyclohexylpiperidyl-3,4-[3H]-(n) ([3H]-TCP) from its binding site with an IC50 of 36 μM suggesting that budipine acts as a non-competitive NMDA antagonist with moderate receptor affinity. It is concluded that the newly discovered NMDA antagonistic action of budipine is at least partly responsible for its antiparkinsonian activity. Our findings are additional evidence for the hypothesis that NMDA antagonists may be useful in the treatment of Parkinson's disease (PD).

Keywords

Budipine NMDA receptor Parkinson's disease 

Copyright information

© Springer-Verlag 1993

Authors and Affiliations

  • T. Klockgether
    • 3
  • P. Jacobsen
    • 1
  • P. -A. Löschmann
    • 2
  • L. Turski
    • 2
  1. 1.CNS DivisionNovo Nordisk A/SM⇘løvDenmark
  2. 2.Research Laboratories of Schering AGBerlinFederal Republic of Germany
  3. 3.Department of NeurologyUniversity of TübingenTübingenFederal Republic of Germany

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