Document Report Card

ID: ALA1125661

Journal: J Med Chem

Title: 2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.

Authors: Ueeda M, Thompson RD, Arroyo LH, Olsson RA.

Abstract: A Langendorff guinea pig heart preparation served for the assay of agonist activity of a series of 24 2-alkoxyadenosines at the A1 and A2 adenosine receptors of, respectively, the atrioventricular node (conduction block) and coronary arteries (vasodilation). Activities are low at the A1 receptor and do not show a clear relationship to the size or hydrophobicity of the C-2 substituent. All the analogues are more potent at the A2 receptor, activity varying directly with the size and hydrophobicity of the alkyl group. The most potent analogue in this series, 2-(2-cyclohexylethoxy)adenosine has an EC50 of 1 nM for coronary vasodilation and is 8700-fold selective for the A2 receptor.

CiteXplore: 2016707

DOI: 10.1021/jm00108a014