Exploring distal regions of the A(3) adenosine receptor binding site: sterically constrained N(6)-(2-phenylethyl)adenosine derivatives as potent ligands

We synthesized phenyl ring-substituted analogues of N(6)-(1S,2R)-(2-phenyl-1-cyclopropyl)adenosine, which is highly potent in binding to the human A(3)AR with a K(i) value of 0.63 nM. The effects of these structural changes on affinity at human and rat adenosine receptors and on intrinsic efficacy a...

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Published in:Bioorg Med Chem
Main Authors: Tchilibon, Susanna, Kim, Soo-Kyung, Gao, Zhan-Guo, Harris, Brian A., Blaustein, Joshua B., Gross, Ariel S., Duong, Heng T., Melman, Neli, Jacobson, Kenneth A.
Format: Artigo
Language:Inglês
Published: 2004
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Article
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC4667970/
https://ncbi.nlm.nih.gov/pubmed/15080906
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2004.02.037
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