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

Article Details

Citation

Copy to clipboard

Ueeda M, Thompson RD, Arroyo LH, Olsson RA

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

J Med Chem. 1991 Apr;34(4):1334-9.

PubMed ID

2016707 [ View in PubMed

]

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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Adenosine	Adenosine receptor A1	EC 50 (nM)	3.39E+03	N/A	N/A	Details