Preladenant (MK-3814; SCH420814)

Description: Preladenant (formerly known as SCH-420814) is a novel potent, selective and competitive antagonist of adenosine A2A receptor with Ki of 0.6 nM and has > 1000-fold selectivity over all other adenosine receptors. It was being investigated in a phase 2 trial for the treatment for Parkinson's disease but did not achieve the expected efficacy. Preladenant (1 mg/kg) inhibited L-Dopa-induced behavioral sensitization after repeated daily administration, which suggests a reduced risk of the development of dyskinesias. Finally, preladenant and SCH 412348 exhibited antidepressant-like profiles in models of behavioral despair, namely the mouse tail suspension test and the mouse and rat forced swim test.

References: Brain Res Bull. 2013 Sep; 98:163-9; ACS Chem Neurosci. 2011 Oct 19; 2(10): 555–567.