SCH-442416 is a selective adenosine A2A receptor antagonist. SCH-442416 binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). It displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM).
Adenosine receptors are a family of GPCRs containing four subtypes (A1 , A2A , A2B and A3 receptors), all of which bind the ubiquitous nucleoside adenosine.[1]. Adenosine is a potent regulator of inflammation. Adenosine mediates its effects on inflammatory cells by engaging one or more cell-surface receptors[2]. SCH442416 is a potent, selective and brain-penetrant antagonist of adenosine A2A receptor (A2AR), with Kis of 0.048 and 0.5 nM for human and rat A2AR respectively[3]. SCH442416 displays more than 23000-fold selectivity over A1R, A2BR, and A3R (Ki=1111, 10000, and 10000 nM, respectively). It can be used for imaging of adenosine A2A receptors in rat and primate brain[4].
SCH-442416 (0.017 mg/kg; i.p.) completely abrogates the CGS-21680-induced decrease in skeletal muscle injury[5]. SCH442416 (1 μM) significantly attenuates the adenosine-induced dilation (from 15.3 to 5.6 μm)[6].
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