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Description: Vipadenant (formerly known as BIIB-014 and CEB-4520) is a novel potent, selective and orally bioaactive antagonist of adenosine A2A receptor with Kis of 1.3 nM and 68 nM for A2A and A1 respectively. Vipadenant is under investigation for for treating Parkinson's disease. Vipadenant was evaluated in phase II clinical trials. Vipadenant showed excellent binding affinity for A2A and had modest selectivity against A1 and A2B (Ki = 63 nM), while it showed good selectivity against A3 (Ki = 1005 nM). When tested in vivo in the mouse and rat haloperidol-induced hypolocomotion models, 44 had a minimum effective dose of 0.1 and 1 mg/kg, respectively.
References: Brain Res Bull. 2013 Sep; 98:163-9; ACS Chem Neurosci. 2011 Oct 19; 2(10): 555–567.
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