Vipadenant is an adenosine antagonist with Ki of 1.3 nM and 68 nM for A2A and A1, respectively. Vipadenant is a selective A2A receptor antagonist with Ki values of 1.3, 68, 63, and 1,005 nM for A2A, A1, A2B, and A3 receptors, respectively, used in development for for Parkinson's disease.
Vipadenant is a selective Adenosine A2A receptor with Ki value of 1.3nM. It exhibits much lower affinity to A1 and A2B with Ki value of 63nM, and Ki value of 1005nM for A3. Vipadenant had a minimum effective dose of 0.1 and 1 mg/kg in the mouse and rat haloperidol-induced hypolocomotion models in vivo, respectively. Vipadenant was able to increase contralateral rotations in 6-OHDA lesioned rats when dosed orally in combination with apomorphine at 3 and 10 mg/kg. Vipadenant also showed reversal of motor disability in MPTP-treated marmosets without dyskinesias at a minimum effective dose of <5 mg/kg, p.o.[1].
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