Long-term L-dopa treatment of Parkinson's disease can lose its effectiveness and cause development of motor complications such as dyskinesia. Furthermore, L-dopa therapy does not address the fundamental pathological process of dopaminergic neurodegeneration in Parkinson's disease. This prompts a search for an alternative or complementary therapy for Parkinson's disease to overcome these limitations. During the last 5 years, the adenosine A(2A) receptor has emerged as an attractive target for Parkinson's disease therapy, primarily because of its localized expression in striatum and motor enhancement function. Recent genetic and pharmacological studies indicate that A(2A) receptor antagonists also offer neuroprotective effects and may possibly modify chronic L-dopa-induced maladaptive responses in animal models of Parkinson's disease. This review summarizes multiple potential benefits of the A(2A) receptor blockade in treating the motor symptoms as well as the underlying dopaminergic neurodegeneration of Parkinson's disease.