tcsc0359 Tozadenant

Tozadenant is an adenosine A_2A receptor antagonist, with K_i of 11.5 nM on human A_2A and 6 nM on rhesus A_2A.

IC50 & Target: Ki: 6 nM (Rhesus A_2A), 11.5 nM (Human A_2A)

In Vivo: ¹⁸F-MNI-444 regional uptake is consistent with A2A receptor distribution in the brain. Selectivity is demonstrated by dose-dependent blocking by tozadenant (1.5, 10.5 mg/kg) and preladenant^[1].