Istradefylline

Istradefylline is a competitive inhibitor of adenosine A2A receptors that exhibits tremorlytic activity. Istradefylline is currently under examination as a potential treatment for Parkinson's disease, as it decreases "off" time in subjects with Parkinson's disease without worsening dyskinesia. Istradefylline increases dopamine levels in normal and 6-OHDA-lesioned animal models, improving cognitive performance. In other animal models, istradefylline decreases GABA release and elicits conditioned place preference (CPP) and increases locomotor activity, indicating a potential role for adenosine receptors in reward and reinforcement.