Taminadenant is a potent, orally active A2AR antagonist.Taminadenant antagonises A2AR agonist-mediated cAMP accumulation and impedance responses with Kb values of 72.8 nM and 8.2 nM, respectively.Taminadenant reverses dyskinesia in several rat models of dyskinesia, including catalepsy, tremor, and hemiparkinsonism. Parkinson's disease. Taminadenant also inhibits tumour growth when combined with Spartalizumab.Taminadenant reactivates anti-tumour immune responses[1][2].Taminadenant did not show any agonist efficacy in HEK cells permanently expressing human A2ARSNAP, but it completely antagonised agonist-mediated cAMP accumulation with an IC50 of 72.8 ± 17.4 nM in HEK cells expressing A2ARSNAP[1].
Taminadenant 动物研究
Animal study
Administered as a single oral dose at 0.3, 3, 7.5, 10 or 30 mg/kg, Taminadenant attenuated the hypnotic effects of Haloperidol in Sprague-Dawley rats, attenuated pilocarpine-induced tremulous jaw movements, and potentiated L-DOPA, showing potent antiparkinsonian activity and possesses antimotor properties[1].
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