848188-19-2Relevant academic research and scientific papers
2,3-Diarylthiophenes as selective EP1 receptor antagonists
Ducharme, Yves,Blouin, Marc,Carriere, Marie-Claude,Chateauneuf, Anne,Cote, Bernard,Denis, Danielle,Frenette, Richard,Greig, Gillian,Kargman, Stacia,Lamontagne, Sonia,Martins, Evelyn,Nantel, Francois,O'Neill, Gary,Sawyer, Nicole,Metters, Kathleen M.,Friesen, Richard W.
, p. 1155 - 1160 (2007/10/03)
The synthesis and the EP1 receptor binding affinity of 2,3-diarylthiophene derivatives are described. The evaluation of the structure-activity relationship (SAR) in this series led to the identification of compounds 4, 7, and 12a, which exhibit high affinity for the human EP 1 receptor and a selectivity greater than 100-fold against the EP2, EP3, EP4, DP, FP, and IP receptors and greater than 25-fold versus the TP receptor. These three antagonists present good pharmacokinetics in rats and significant differences in the way they are distributed in the brain.
