Synthesis and biological evaluation of allosteric A1-adenosine receptor modulators structurally related to (2-amino-4,5,6,7-tetrahydro-benzo[b]thiophen-3-yl)-(4-chloro-phenyl)-miethanone, a potent compound useful to reduce neuropathic pain
Synthesis and biological evaluation of allosteric A1-adenosine receptor modulators structurally related to (2-amino-4,5,6,7-tetrahydro-benzo[b]thiophen-3-yl)-(4-chloro-phenyl)-miethanone, a potent compound useful to reduce neuropathic pain
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DOI：
10.1007/s00044-005-0129-8
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发表时间：
2005-01-01
影响因子：
2.6
通讯作者：
Borea, PAA
中科院分区：
文献类型：
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作者：
Romagnoli, R;Baraldi, PG;Borea, PAA
合成了新的（2-氨基-4,5,6,7-四氢苯[b]噻吩-3-基）-（4-氯苯基）甲烷酮衍生物（化合物1），这是一种与A(1)-腺苷受体结合的激动剂的变构增强剂，并在不同浓度的完整细胞实验中进行了评估，以确定其中哪些是腺苷激活人- 1腺苷受体的潜在变构增强剂。在10 μ m浓度下，合成的化合物没有一种比1更有效，大多数化合物增加表达人a(1)-腺苷受体的CHO细胞的cAMP含量，表明具有拮抗剂活性。只有两种化合物（2和8）在高浓度（10 μ M）下表现为变构增强剂。
New derivatives of (2-amino-4,5,6,7-tetrahydrobenzo[b]thiophen-3-yl)-(4-chlorophenyl)methanone (compound 1), an allosteric enhancer of agonist binding to the A(1)-adenosine receptor, have been synthesized and evaluated in an intact cell assay at different concentrations to determine which among them were potential allosteric enhancers of the action of adenosine to activate the human-A(1)adenosine receptor. None of the synthesized compounds appear to be more potent than 1 at a concentration of 10 mu M. Most of the compounds increase the cAMP content of CHO cells expressing the human A(1)-adenosine receptor, indicating an antagonist activity. Only two of the evaluated compounds (2 and 8) appeared to be allosteric enhancers at high concentration (10 mu M).