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Biol. , 277, 19056, 2002. 24. S. , N6-substituted D-4′-thioadenosine-5′-methyluronamides: potent and selective agonists at the human A3 adenosine receptor, J. Med. , 46, 3775, 2003. 25. A. , Methanocarba analogues of purine nucleosides as potent and selective AR agonists, J. Med. , 43, 2196, 2000. 26. Lee, K. , Ring-constrained (N)-methanocarba nucleosides as adenosine receptor agonists: independent 5′-uronamide and 2′-deoxy modifications, Bioorg. Med. Chem. , 11, 1333, 2001. 27. Tchilibon, S. , (N)-methanocarba 2,N6-disubstituted adenine nucleosides as highly potent and selective A3 adenosine receptor agonists, J.

The A1, A2A, and A2B receptors (>10,000-fold) ever reported. 7 PYRAZOLOQUINOLINES The 2-aryl-pyrazolo [4,3-c] quinolin-4-one skeleton was recently reported as a template for selective A3AR antagonists. 0 nM. fm Page 32 Wednesday, May 24, 2006 3:00 PM 32 Adenosine Receptors were also identified in a library of compounds described earlier as a source of A3AR antagonists. 9 THIAZOLES AND THIADIAZOLES Thiazole and thiadiazole analogs 75–79 were first identified as a promising class of compounds after the screening of several 5- and 6-membered heterocyclic core templates to replace isoquinoline and quinazoline skeletons for new adenosine receptor antagonists.

76. G. , Structural determinants of efficacy at A3 adenosine receptors: modification of the ribose moiety, Biochem. , 67, 893, 2004. 77. G. , Allosterism in membrane receptors, Drug Disc. Today, 11, 191, 2006. 78. Ramkumar, V. , The A3 adenosine receptor is the unique adenosine receptor which facilitates release of allergic mediators in mast cells, J. Biol. , 268, 16887, 1993. fm Page 39 Tuesday, June 20, 2006 10:56 AM 3 The Role of CD73 in the Generation of Extracellular Adenosine for Adenosine Receptor Signaling Masahide Takedachi, Sean P.

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