Istradefylline has 70-fold greater affinity for the A2AR than the A1 receptor with Ki of 2.2 nM versus 150 nM. Istradefylline causes concentration-dependent abolition of bFGF induction of astrogliosis in primary rat striatal astrocytes. Istradefylline binds to A1 receptor, A2A receptor, and A3 receptor in human with Kis of >287 nM, 9.12 nM, and >681 nM, respectively, 50.9 nM and 1.57 nM for A1 receptor and A2A receptor in rat, 105.02 nM and 1.87 nM for A1 receptor and A2A receptor in mouse, respectively.