R. Romagnoli, P. Baraldi, M. Pavani
Apr 1, 2005
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Medicinal Chemistry Research
Abstract
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 A1-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-A1 adenosine receptor. None of the synthesized compounds appear to be more potent than 1 at a concentration of 10 μM. Most of the compounds increase the cAMP content of CHO cells expressing the human A1-adenosine receptor, indicating an antagonist activity. Only two of the evaluated compounds (2 and 8) appeared to be allosteric enhancers at high concentration (10 μM).