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The novel adenosine A2a antagonist ST1535 potentiates the effects of a threshold dose of l-dopa in unilaterally 6-OHDA-lesioned rats.

Abstract
Adenosine A2a antagonists can modulate dopamine-mediated motor behaviours, however, their ability to induce rotational behaviour in 6-hydroxydopamine (6-OHDA)-lesioned rats and to potentiate the effects of l-dopa differs. We now report on the effects of the novel A2a antagonist ST1535 on rotational responses in this model. When administered alone, ST1535 (2.5-40 mg/kg po) enhanced exploratory behaviour and produced a dose-related increase in ipsilateral rotation in rats with a unilateral 6-OHDA lesion of the nigro-striatal pathway. Administration of ST1535 (40 mg/kg po) in combination with a high dose of l-dopa (12 mg/kg ip) caused marked contraversive rotation but did not alter the rotational response produced by l-dopa alone. In contrast, when administered in combination with l-dopa (7 mg/kg ip) that alone produced a submaximal circling response, ST1535 enhanced the intensity and duration of rotation. These results suggest that ST1535 is able to alter dopamine-mediated behaviour when given alone and to potentiate the effects of submaximal doses of l-dopa. ST1535 may be useful in the treatment of Parkinson's disease and effective in reducing the use of l-dopa.
AuthorsSarah Rose, Neil Ramsay Croft, Peter Jenner
JournalBrain research (Brain Res) Vol. 1133 Issue 1 Pg. 110-4 (Feb 16 2007) ISSN: 0006-8993 [Print] Netherlands
PMID17196564 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 2-n-butyl-9-methyl-8-(1,2,3)triazol-2-yl-9H-purin-6-ylamine
  • Adenosine A2 Receptor Antagonists
  • Dopamine Agents
  • Receptor, Adenosine A2A
  • Sympatholytics
  • Triazoles
  • Levodopa
  • Oxidopamine
  • Adenine
  • Adenosine
Topics
  • Adenine (analogs & derivatives, pharmacology)
  • Adenosine (metabolism)
  • Adenosine A2 Receptor Antagonists
  • Animals
  • Brain (drug effects, metabolism, physiopathology)
  • Disease Models, Animal
  • Dopamine Agents (pharmacology)
  • Dose-Response Relationship, Drug
  • Drug Synergism
  • Exploratory Behavior (drug effects, physiology)
  • Levodopa (pharmacology)
  • Male
  • Movement (drug effects, physiology)
  • Oxidopamine
  • Parkinsonian Disorders (drug therapy, metabolism, physiopathology)
  • Rats
  • Rats, Wistar
  • Receptor, Adenosine A2A (metabolism)
  • Sympatholytics
  • Triazoles (pharmacology)

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