CAY10498

The A₁, A_2A, A_2B, and A₃ adenosine receptors (ARs) are ubiquitous G protein-coupled receptors. The four AR subtypes have been implicated in several areas of therapeutic interest such as stroke and other ischemic conditions, as well as inflammation, neurodegenerative diseases, diabetes, and sleep regulation.¹ A₃ AR antagonists are of interest as therapeutic agents in glaucoma agents and inflammation. CAY10498 is a potent and selective A₃ AR antagonist exhibiting a K_i of 37 nM with 60 and 200-fold selectivity over A₁ and A_2A adenosine receptors, respectively.¹ CAY10498 is also a structural analog of reversine, a dedifferentiation agent of embryonic progenitor cells.² However, no dedifferentiation effects or any connection between A₃ AR antagonism and dedifferentiation have been demonstrated.

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1. Perreira, M., Jiang, J.K., Klutz, A.M., et al. "Reversine" and its 2-substituted adenine derivatives as potent and selective A₃ adenosine receptor antagonists. J. Med. Chem. 48(15), 4910-4918 (2005).

2. Chen, S., Zhang, Q., Wu, X., et al. Dedifferentiation of lineage-committed cells by a small molecule. J. Am. Chem. Soc. 126(2), 410-411 (2004).