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[摘要]：Purine nucleoside derivatives that are selective ligands for the A(3) adenosine receptor (AR) hove been structurally modified such that their ability to activate the receptor is lost while retaining high binding affinity This loss of efficacy in otherwise selectively binding nucleosides has been shown to result in antagonism of the effects of known agonists in functional assays Modification of the ribose moiety has been the most effective strategy to accomplish this aim Steric constraints have been introduced, as well as replacement of the various hydrogen bond-donating groups, to achieve a reduction in efficacy High selectivity has recently been achieved for such nucleoside-based A(3) AR antagonists Thus, it is now possible to compare nucleoside-based A(3) antagonists with well-characterized heterocyclic nonpurine antagonists as clinical candidates for the treatment of glaucoma, asthma and inflammation |
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