Truncated (N)-Methanocarba Nucleosides as Partial Agonists at Mouse and Human A(3) Adenosine Receptors: Affinity Enhancement by N(6)-(2-Phenylethyl) Substitution

Dopamine-derived N(6)-substituents, compared to N(6)-(2-phenylethyl), in truncated (N)-methanocarba (bicyclo[3.1.0]hexyl) adenosines favored high A(3) adenosine receptor (AR) affinity/selectivity, e.g. C2-phenylethynyl analogue 15 (MRS7591, K(i) 10.9/17.8 nM, at human/mouse A(3)AR). 15 was a partial...

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Published in:J Med Chem
Main Authors: Tosh, Dilip K., Salmaso, Veronica, Rao, Harsha, Bitant, Amelia, Fisher, Courtney L., Lieberman, David I., Vorbrüggen, Helmut, Reitman, Marc L., Gavrilova, Oksana, Gao, Zhan-Guo, Auchampach, John A., Jacobson, Kenneth A.
Format: Artigo
Language:Inglês
Published: 2020
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC7443318/
https://ncbi.nlm.nih.gov/pubmed/32271569
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.0c00235
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