Taminadenant

Taminadenant (NIR178; PBF509) is a highly potent and orally active adenosine A_2A receptor (A_2AR) antagonist. Taminadenant can antagonize A2AR agonist-mediated cAMP accumulation and impedance responses with K_B values of 72.8 nM and 8.2 nM, respectively. Taminadenant reverses motor impairments in several rat models of movement disorders, including catalepsy, tremor, and hemiparkinsonism. Taminadenant can also inhibit tumor growth when combined with Spartalizumab (HY-P9972). Taminadenant reactivate the antitumor immune response^[1][2]. IC50 & Target:Adenosine receptor^[1] In Vitro:Taminadenant (PBF509) does not show any agonist efficacy in HEK cells permanently expressing the human A_2AR^SNAP, but completely antagonizes the agonist-mediated cAMP accumulation in A_2AR^SNAP expressing HEK cells with an IC₅₀ of 72.8 ± 17.4 nM^[1]. In Vivo:Taminadenant (PBF509) (0.3, 3, 7.5, 10, or 30 mg/kg; p.o.; single dosage) attenuates the cataleptic effects of Haloperidol, attenuates pilocarpine-induced tremulous jaw movement, enhances the effects of L-DOPA, shows a robust antiparkinsonian activity and displays antidyskinetic efficacy^[1].