Structure-activity relationships for N6-substituted adenosines at a brain A1-adenosine receptor with a comparison to an A2-adenosine receptor regulating coronary blood flow.

阅读量:

35

作者:

RD Thompson

展开

摘要:

A series of 145 N 6-substituted adenosines have been screened as inhibitors of the binding of [ 3H]cyclohexyladenosine to an A 1-adenosine receptor in rat brain membranes and the results compared to the potencies of these analogs in increasing coronary blood flow via activation of an A 2-adenosine receptor. The A 1 receptor shows greater stereoselectivity in the N 6 region of the receptor towards asymmetric aralkyl substituents, and shows greater bulk tolerance in the N 6 region such that it retains affinity for certain N 6-tertiary alkyladenosines and N 6-cycloalkyladenosines that are inactive at the coronary A 2 receptor. At the A 1 receptor, the most potent analogs have either aliphatic N 6-substituents with four or more methylene residues or have an N 6-halophenyl substituent. At the A 2 receptor, the most potent analogs have an N 6-phenethyl or similar heteroarylethyl substituent. Certain sets or series of analogs appear useful for identifying the subtypes of adenosine receptors involved in physiological functions.

展开

DOI:

10.1016/0006-2952(86)90042-0

被引量:

385

年份:

1986

通过文献互助平台发起求助,成功后即可免费获取论文全文。

我们已与文献出版商建立了直接购买合作。

你可以通过身份认证进行实名认证,认证成功后本次下载的费用将由您所在的图书馆支付

您可以直接购买此文献,1~5分钟即可下载全文,部分资源由于网络原因可能需要更长时间,请您耐心等待哦~

身份认证 全文购买

相似文献

参考文献

引证文献

来源期刊

Biochemical Pharmacology
1 August 1986

引用走势

2012
被引量:30

辅助模式

0

引用

文献可以批量引用啦~
欢迎点我试用!

引用