preladenant

Preladenant is a potent and highly selective small molecule antagonist of the adenosine A₂A receptor (ADORA2A). It was originally developed by Schering-Plough and later by Merck & Co following acquisition of Schering-Plough. Preladenant was investigated as an oral treatment for Parkinson's disease and other movement disorders due to its ability to modulate neuronal activity in the basal ganglia via antagonism of the A₂A receptor—a target implicated in motor control. The drug demonstrated positive results in Phase II clinical trials but failed to show efficacy over placebo in Phase III trials and development was discontinued in May 2013. Preladenant has very high affinity for the A₂A receptor (Ki ≈ 1 nM), with over 1000-fold selectivity compared to other adenosine receptors. In animal models and early human studies it improved motor function without worsening dyskinesia when used alone or as adjunctive therapy with levodopa[1][6][7].

Other names

preladenantum5-Amino-2-(2-furanyl)-7-[2-[4-[4-(2-methoxyethoxy)phenyl]-1-piperazinyl]ethyl]-7H-pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidine4-(furan-2-yl)-10-[2-[4-[4-(2-methoxyethoxy)phenyl]piperazin-1-yl]ethyl]-3,5,6,8,10,11-hexazatricyclo[7.3.0.02,6]dodeca-1(9),2,4,7,11-pentaen-7-amine7H-Pyrazolo(4,3-e)(1,2,4)triazolo(1,5-c)pyrimidin-5-amine 2-(2-furanyl)-7-(2-(4-(4-(2-methoxyethoxy)phenyl)-1-piperazinyl)ethyl)