Adenosine A2A receptor antagonists exert motor and neuroprotective effects by distinct cellular mechanisms

Ann Neurol. 2008 Mar;63(3):338-46. doi: 10.1002/ana.21313.

Abstract

Objective: To investigate whether the motor and neuroprotective effects of adenosine A(2A) receptor (A(2A)R) antagonists are mediated by distinct cell types in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) model of Parkinson's disease.

Methods: We used the forebrain A(2A)R knock-out mice coupled with flow cytometric analyses and intracerebroventricular injection to determine the contribution of A(2A)Rs in forebrain neurons and glial cells to A(2A)R antagonist-mediated motor and neuroprotective effects.

Results: The selective deletion of A(2A)Rs in forebrain neurons abolished the motor stimulant effects of the A(2A)R antagonist KW-6002 but did not affect acute MPTP neurotoxicity. Intracerebroventricular administration of KW-6002 into forebrain A(2A)R knock-out mice reinstated protection against acute MPTP-induced dopaminergic neurotoxicity and attenuated MPTP-induced striatal microglial and astroglial activation.

Interpretation: A(2A)R activity in forebrain neurons is critical to the control of motor activity, whereas brain cells other than forebrain neurons (likely glial cells) are important components for protection against acute MPTP toxicity.

Publication types

  • Comparative Study
  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, Non-P.H.S.

MeSH terms

  • Adenosine A2 Receptor Antagonists*
  • Animals
  • MPTP Poisoning / drug therapy
  • MPTP Poisoning / prevention & control
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Mice, Transgenic
  • Motor Activity / drug effects
  • Motor Activity / physiology*
  • Neuroglia / cytology
  • Neuroglia / drug effects
  • Neuroglia / physiology
  • Neurons / cytology*
  • Neurons / drug effects
  • Neurons / physiology
  • Neuroprotective Agents / pharmacology*
  • Neuroprotective Agents / therapeutic use
  • Prosencephalon / cytology
  • Prosencephalon / drug effects
  • Prosencephalon / physiology
  • Purines / pharmacology
  • Purines / therapeutic use
  • Receptor, Adenosine A2A / deficiency
  • Receptor, Adenosine A2A / physiology

Substances

  • Adenosine A2 Receptor Antagonists
  • Neuroprotective Agents
  • Purines
  • Receptor, Adenosine A2A
  • istradefylline