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- W2019944766 abstract "A series of trisubstituted purinones was synthesized and evaluated as A2A receptor antagonists. The A2A structure–activity relationships at the three substituted positions were studied and selectivity against the A1 receptor was investigated. One antagonist 12o exhibits a Ki of 9 nM in an A2A binding assay, a Kb of 18 nM in an A2A cAMP functional assay, and is 220-fold selective over the A1 receptor." @default.
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- W2019944766 date "2009-03-01" @default.
- W2019944766 modified "2023-10-13" @default.
- W2019944766 title "Synthesis and SAR studies of trisubstituted purinones as potent and selective adenosine A2A receptor antagonists" @default.
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- W2019944766 doi "https://doi.org/10.1016/j.bmcl.2009.01.042" @default.
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