| References: |
BAY-545 is a novel, potent and selective antagonist of A2B adenosine receptor with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2Badenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor. The A2B adenosine receptor is a G protein-coupled receptor that belongs to the four member family of adenosine receptors: A1, A2A, A2B, A3. While adenosine-mediated A2B receptor signaling attenuates acute inflammation, facilitates tissue adaptation to hypoxia, and induces increased ischemia tolerance under conditions of an acute insult, persistently elevated adenosine levels and A2B receptor signaling are characteristics of a number of chronic disease states. |
