A potent, brain-permeable, and selective A2AR antagonist; selective for A2AR over A1R, A2BR, and A3R (Kis = 0.048, 1,111, >10,000, and >10,000 nM, respectively) using human recombinant receptors; selective for A2AR over A1R and A3R in rat cerebral membranes (Kis = 0.50, 1,815, and >10,000 nM, respectively); is taken up preferentially by liver, adrenal gland, kidney, and lungs, and by the striatum in the brain; attenuates adenosine-mediated and A2AR agonist-induced arteriole dilation at a concentration of 10 μM