Allosteric Modulators of the Adenosine A1Receptor: Synthesis and Pharmacological Evaluation of 4-Substituted 2-Amino-3-benzoylthiophenes
Journal of Medicinal Chemistry2009Vol. 52(14), pp. 4543–4547
Citations Over TimeTop 10% of 2009 papers
Luigi Aurelio, Céline Valant, Bernard L. Flynn, Patrick M. Sexton, Arthur Christopoulos, Peter J. Scammells
Abstract
A series of 4-substituted 2-amino-3-benzoylthiophenes was screened using a functional assay of A1AR-mediated phosphorylation of ERK1/2 in intact CHO cells to identify both potential agonistic effects as well the ability to allosterically modulate the activity of the orthosteric agonist, R-PIA. More detailed concentration−response experiments were subsequently performed on two compounds (9a and 9o) utilizing both the ERK1/2 assay as well as a second assay of [35S]GTPγS binding to activated G proteins.
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