Activation of the Gi protein-coupled A3 adenosine receptor (AR) is associated with anticancer, antiischemic and antiinflammatory effects, and clinical trials of several prototypical selective agonists are underway. See, for example, Ochaion, A., et al., Cell Immunol. 2009, 258:115-122; and Cohen, S., et al., J. Cell. Physiol. 2011, 226: 2438-2447. A3AR antagonists are being examined as promising agents for the treatment of glaucoma. Wang, Z., et al., Exp. Eye Res. 2010, 90:146-154; and Okamura, T., et al., Bioorg. Med. Chem Lett. 2004, 14: 3775-3779. Characterization of the A3AR in tissues and assays to establish a structure-activity relationship (SAR) of newly synthesized compounds for drug discovery, as for many other G protein-coupled receptors (GPCRs), is often dependent on the use of high affinity radioligands.
FLUORESCENT ANTAGONISTS OF THE A3 ADENOSINE RECEPTOR
SPALLUTO, GIAMPIERO;MORO, STEFANO
2012-01-01
Abstract
Activation of the Gi protein-coupled A3 adenosine receptor (AR) is associated with anticancer, antiischemic and antiinflammatory effects, and clinical trials of several prototypical selective agonists are underway. See, for example, Ochaion, A., et al., Cell Immunol. 2009, 258:115-122; and Cohen, S., et al., J. Cell. Physiol. 2011, 226: 2438-2447. A3AR antagonists are being examined as promising agents for the treatment of glaucoma. Wang, Z., et al., Exp. Eye Res. 2010, 90:146-154; and Okamura, T., et al., Bioorg. Med. Chem Lett. 2004, 14: 3775-3779. Characterization of the A3AR in tissues and assays to establish a structure-activity relationship (SAR) of newly synthesized compounds for drug discovery, as for many other G protein-coupled receptors (GPCRs), is often dependent on the use of high affinity radioligands.Pubblicazioni consigliate
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