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Preladenant

Preladenant (developmental code name SCH-420814) is a drug that was developed by Schering-Plough which acts as a potent and selective antagonist of the adenosine A<sub>2A</sub> receptor. It was being researched as a potential treatment for Parkinson's disease. Positive results were reported in Phase II clinical trials in humans, but it did not prove itself to be more effective than a placebo during Phase III trials, and so was discontinued in May 2013.

The drug has very high affinity for the A<sub>2A</sub> receptor (<1nM) and shows more than 1,000-fold selectivity for the A<sub>2A</sub> receptor over the other adenosine receptors.

Preladenant shows pro-motivational effects in animals and reverses tetrabenazine-induced motivational deficits. Other A<sub>2A</sub> receptor antagonists, including istradefylline, Lu AA47070, MSX-3, and MSX-4, have also shown such effects. These agents may be useful in the treatment of motivational disorders in humans. Accordingly, istradefylline has been reported to reduce apathy, anhedonia, fatigue, and depression in people with Parkinson's disease.

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