ASP5854 (ASP-5854) is a potent adenosine A(1) and A(2A) receptor dual antagonist with binding Ki of 9.03 and 1.76 nM for human A(1) and A(2A) receptors, respectively.
ASP5854 displays high specificity over adenosine A3 receptor, and shows similar binding affinity for A1 and A2A receptors in humans, rats, and mice.
ASP5854 showed antagonistic action on A(1) and A(2A) agonist-induced (CPA, CGS21680) increases of intracellular Ca(2+) concentration with IC50 of 59.81 and 4.21 nM, respectively.
ASP5854 significantly potentiated l-dihydroxyphenylalanine (L-DOPA)-induced rotational behavior at doses higher than 0.032 mg/kg in unilateral 6-hydroxydopamine-lesioned rats.
ASP5854 significantly reversed the scopolamine-induced memory deficits in the rat passive avoidance test, but the specific adenosine A(2A) antagonist KW-6002 (istradefylline, Cat#PC-42728) did not.
ASP5854 ameliorated MK-801-induced impairment of spontaneous alternation in the mouse Y-maze test, but not KW-6002 (istradefylline, Cat#PC-42728).