2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.
2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.
复制标题
2-烷氧基腺苷：冠状动脉 A2 腺苷受体的有效选择性激动剂。
DOI：
10.1021/jm00108a014
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发表时间：
1991
影响因子：
7.3
通讯作者：
Olsson,RA
中科院分区：
文献类型：
--
作者：
Ueeda,M;Thompson,RD;Arroyo,LH;Olsson,RA
A Langendorff guinea pig heart preparation served for the assay of agonist activity of a series of 24 2-alkoxyadenosines at the Aj and A2 adenosine receptors of, respectively, the atrioventricular node (conduction block) and coronary arteries (vasodilation). Activities are low at the At 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 inthis series, 2-(2-cyclohexylethoxy) adenosine, has an EC50 of 1 nM for coronary vasodilation and is 8700-fold selective for the A2 receptor.Exocyclic substituents on the adenine base profoundly alter the affinity of adenosine for its receptors,^-sub-stituted adenosines such as A^-cyclopentyladenosine1· 2 are potent and very selective agonists at the At adenosine receptor (A1AR). 3, 4 Certain other N-6 substituents con-taining aryl groups confer selectivityfor the A2AR. 5, 6 The availability of large numbers of N6-substituted adenosines has aidedthe development of models of the N-6 region of
