Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor
Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor
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DOI：
10.1016/s0960-894x(00)00379-6
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发表时间：
2000-09-04
影响因子：
2.7
通讯作者：
Romagnoli, R
中科院分区：
文献类型：
--
作者：
Baraldi, PG;Zaid, AN;Romagnoli, R
PD 81，723是一种与A（1）-腺苷受体结合的激动剂的变构增强剂，其新衍生物已被合成并在完整细胞试验中进行了评估。化合物3a、3 o和3 p似乎比PD 81.723更有效，并且在0.1 μ M的浓度下引起表达人A（1）-腺苷受体的CHO细胞的cAMP含量的显著降低。化合物4 e和4 o在低浓度下似乎是变构增强剂，在较高浓度下似乎是拮抗剂，而化合物3c、3g、3s和111似乎是弱拮抗剂，在10 μ M的较高浓度下也是变构增强剂。(C)2000爱思唯尔科技有限公司版权所有。
New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A(1)-adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds 3a, 3o and 3p appeared to be more potent than PD 81.723 and at a concentration of 0.1 mu M caused significant reductions of cAMP content of CHO cells expressing the human A(1)-adenosine receptor. Compounds 4e and 4o appeared to be allosteric enhancers at a low concentration and antagonists at a higher concentration, whereas compounds 3c, 3g, 3s and ill appeared to be weak antagonists that are also allosteric enhancers at the: higher concentration of 10 mu M. (C) 2000 Elsevier Science Ltd. All rights reserved.