The primary pathology of Parkinson's disease is the degeneration of dopaminergic neurons in the nigrostriatal pathway, resulting in a significant reduction in striatum dopamine concentration which is responsible for the altered motor functions. With time and disease progression, efficacy of dopaminergic therapy becomes unpromising. Since adenosine A2A receptor is selectively localized in striatum for controlling motor activity, it appeared to be an attractive target for a novel treatment in Parkinson's disease. Several lines of evidence indicated that KW-6002, highly selective antagonist of adenosine A2A receptor, showed anti-parkinsonian effect in vivo and in vitro without any problematic side effect which is observed in dopaminergic therapy. Further investigation will be necessary to make sure the effect in ongoing progressive nature of Parkinson's disease or the long treatment periods in Parkinson's disease.