Document Report Card
Basic Information
ID: ALA1133137
Journal: Bioorg Med Chem Lett
Title: Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor.
Authors: Baraldi PG, Zaid AN, Lampronti I, Fruttarolo F, Pavani MG, Tabrizi MA, Shryock JC, Leung E, Romagnoli R.
Abstract: New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1-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 microM caused significant reductions of cAMP content of CHO cells expressing the human A1-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 4l appeared to be weak antagonists that are also allosteric enhancers at the higher concentration of 10 microM.
CiteXplore: 10987425