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Vipadenant is a selective adenosine 2A (A2A) receptor antagonist with Ki values of 1.3, 68, 63, and 1,005 nM for A2A, A1, A2B, and A3 receptors, respectively, in a radioligand binding assay.1 It acts as a functional antagonist of human recombinant A2A (KA = 0.58 nM) in a calcium mobilization-based FLIPR assay. Vipadenant also reverses haloperidol-induced hypolocomotion in mice and rats.
WARNING This product is not for human or veterinary use.
1. Antagonists of the human A2A adenosine receptor. 4. Design, synthesis, and preclinical evaluation of 7-