Mitochondria-targeted antioxidant effects of S(-) and R(+) pramipexole

BMC Pharmacol. 2010 Feb 5:10:2. doi: 10.1186/1471-2210-10-2.

Abstract

Background: Pramipexole exists as two isomers. The S(-) enantiomer is a potent D3/D2 receptor agonist and is extensively used in the management of PD. In contrast, the R(+) enantiomer is virtually devoid of any of the DA agonist effects. Very limited studies are available to characterize the pharmacological spectrum of the R(+) enantiomer of pramipexole.

Results: Using differentiated SH-SY5Y neuroblastoma cells as an experimental model, here we show that S(-) and R(+) pramipexole are endowed with equipotent efficacy in preventing cell death induced by H2O2 and inhibiting mitochondrial reactive oxygen species generation. Both pramipexole enantiomers prevented mitochondrial ROS generation with a potency about ten times higher then that elicited for neuroprotection.

Conclusions: These results support the concept of both S(-) and R(+) pramipexole enantiomers as mitochondria-targeted antioxidants and suggest that the antioxidant, neuroprotective activity of these drugs is independent of both the chiral 6-propylamino group in the pramipexole molecule and the DA receptor stimulation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antioxidants / administration & dosage*
  • Apoptosis / drug effects
  • Benzothiazoles / administration & dosage*
  • Cell Culture Techniques
  • Cell Survival / drug effects
  • Dopamine Antagonists / administration & dosage
  • Drug Delivery Systems
  • Humans
  • Hydrogen Peroxide / toxicity
  • Mitochondria / drug effects*
  • Mitochondria / pathology
  • Neurons / drug effects*
  • Neurons / pathology
  • Neuroprotective Agents / pharmacology
  • Oxidative Stress / drug effects
  • Pramipexole
  • Reactive Oxygen Species / metabolism*
  • Rosiglitazone
  • Thiazolidinediones / pharmacology
  • Tumor Cells, Cultured

Substances

  • Antioxidants
  • Benzothiazoles
  • Dopamine Antagonists
  • Neuroprotective Agents
  • Reactive Oxygen Species
  • Thiazolidinediones
  • Rosiglitazone
  • Pramipexole
  • Hydrogen Peroxide