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