The effect of low oral doses of (-)-deprenyl and its metabolites on DSP-4 toxicity

J Neural Transm (Vienna). 2001;108(11):1239-47. doi: 10.1007/s007020100002.

Abstract

Treatment with a single oral dose of (-)-deprenyl (selegiline) before DSP-4 administration could dose-dependently decrease the noradrenaline (NA) depleting effect of the toxin in mouse hippocampus. The maximum protective effect was achieved at as low oral dose as 0.25 mg/kg. Pre-treatment with the same doses of the main metabolites of (-)-deprenyl; (-)-amphetamine and (-)-methylamphetamine provided a weaker attenuation of DSP-4 induced NA depletion, than the parent compound. The selective noradrenergic toxin DSP-4, which depletes NA in nerve terminals originating from the locus coeruleus, is presumably metabolised by CYP-450 enzymes. Continuous administration of low, by themselves non-toxic doses of DSP-4 resulted in the cumulation of its NA depleting effect.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Antiparkinson Agents / administration & dosage
  • Antiparkinson Agents / metabolism
  • Benzylamines / administration & dosage
  • Benzylamines / toxicity*
  • Dose-Response Relationship, Drug
  • Drug Administration Schedule
  • Hippocampus / drug effects
  • Hippocampus / metabolism
  • Injections, Intraperitoneal
  • Male
  • Mice
  • Monoamine Oxidase Inhibitors / administration & dosage
  • Monoamine Oxidase Inhibitors / metabolism
  • Neurotransmitter Uptake Inhibitors / administration & dosage
  • Neurotransmitter Uptake Inhibitors / toxicity*
  • Norepinephrine / metabolism
  • Selegiline / administration & dosage*
  • Selegiline / metabolism*

Substances

  • Antiparkinson Agents
  • Benzylamines
  • Monoamine Oxidase Inhibitors
  • Neurotransmitter Uptake Inhibitors
  • Selegiline
  • DSP 4
  • Norepinephrine