-methyl-(N )-methanocarba-2Ј-deoxyadenosine-3Ј,5Ј-bisphosphate (MRS2279) was developed previously as a selective high-affinity, non-nucleotide P2Y 1 receptor (P2Y1-R) antagonist
Novel methanocarba adenosine analogues, having the pseudo-ribose northern (N) conformation preferred at adenosine receptors (ARs), were synthesized and tested in binding assays. The 5'-uronamide modification preserved [N6-(3-iodobenzyl)] or enhanced (N6-methyl) affinity at A3ARs, while the 2'-deoxy modification reduced affinity and efficacy in a functional assay.
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