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MRS1220 is an adenosine A3 receptor antagonist (Ki = 0.65 nM for the human receptor).1 It is selective for human adenosine A3 receptors over rat adenosine A1 and A2receptors (Kis = 305 and 52 nM, respectively). MRS1220 inhibits [35S]GTPγS binding in HEK293 cells expressing human adenosine A3 receptors (IC50 = 7.2 nM). In vivo, MRS1220 (0.15 mg/kg) decreases tumor growth and angiogenesis in a rat C6 glioma model.2
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1. Pharmacological characterization of novel A3 adenosine receptor-
2. The adenosine A3 receptor regulates differentiation of glioblastoma stem-