SCH-58261 is a drug which acts as a potent and selective antagonist for the adenosine receptor A_2A, with more than 50x selectivity for A_2A over other adenosine receptors. It has been used to investigate the mechanism of action of caffeine, which is a mixed A₁ / A_2A antagonist, and has shown that the A_2A receptor is primarily responsible for the stimulant effects of caffeine, but blockade of both A₁ and A_2A receptors is required to accurately replicate caffeine's effects in animals. SCH-58261 has also shown antidepressant and neuroprotective effects in a variety of animal models, and has been investigated as a possible treatment for Parkinson's disease.