TY - JOUR
T1 - Allosteric modulators of the adenosine A1 receptor: Synthesis and pharmacological evaluation of 4-substituted 2-amino-3-benzoylthiophenes
AU - Aurelio, Luigi
AU - Valant, Celine
AU - Flynn, Bernard Luke
AU - Sexton, Patrick M
AU - Christopoulos, Arthur
AU - Scammells, Peter John
PY - 2009
Y1 - 2009
N2 - (BRIEF ARTICLE) A series of 4-substituted 2-amino-3-benzoylthiophenes was screened using a functional assay of A(1)AR-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 [(35)S]GTPgammaS binding to activated G proteins.
AB - (BRIEF ARTICLE) A series of 4-substituted 2-amino-3-benzoylthiophenes was screened using a functional assay of A(1)AR-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 [(35)S]GTPgammaS binding to activated G proteins.
UR - http://www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&dopt=Citation&list_uids=19514747
M3 - Article
SN - 0022-2623
VL - 52
SP - 4543
EP - 4547
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
IS - 14
ER -