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A series of trisubstituted purinones was synthesized and evaluated as A(2A) receptor antagonists. The A(2A) structure-activity relationships at the three substituted positions were studied and selectivity against the A(1) receptor was investigated. One antagonist 12o exhibits a K(i) of 9nM in an A(2A) binding assay, a K(b) of 18nM in an A(2A) cAMP functional assay, and is 220-fold selective over the A(1) receptor.


Yuefei Shao, Andrew G Cole, Marc-Raleigh Brescia, Lan-Ying Qin, Jingqi Duo, Tara M Stauffer, Laura L Rokosz, Brian F McGuinness, Ian Henderson. Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists. Bioorganic & medicinal chemistry letters. 2009 Mar 1;19(5):1399-402

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PMID: 19181527

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