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**SCH58261** is a synthetic, small molecule that acts as a potent and highly selective antagonist of the adenosine A2A receptor, showing more than 50-fold selectivity over other adenosine receptor subtypes. Its principal mechanism involves selective blockade of the adenosine A2A receptor, a G protein-coupled receptor widely expressed in the striatum and other brain regions and peripherally in immune tissues. SCH58261 is widely used as a reference compound in preclinical research and has demonstrated antidepressant, nootropic, neuroprotective, and anti-parkinsonian activity in animal models. It is also being explored for its potential to enhance cancer immunotherapy, particularly as a combination partner with immune checkpoint inhibitors. Poor oral bioavailability limits its clinical development, mainly due to poor absorption and high first-pass hepatic metabolism. SCH58261 is classified as a non-xanthine heterocyclic compound and is structurally a triazolopyrimidine derivative[1][2][4][6][7][8][9].
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