Author/Authors :
Hélène Juteau، نويسنده , , Yves Gareau، نويسنده , , Marc Labelle، نويسنده , , Claudio F. Sturino، نويسنده , , Nicole Sawyer، نويسنده , , Nathalie Tremblay، نويسنده , , Sonia Lamontagne، نويسنده , , Marie-Claude Carrière، نويسنده , , Danielle Denis، نويسنده , , Kathleen M. Metters، نويسنده ,
Abstract :
Potent and selective antagonists of the human EP3 receptor have been identified. The structure–activity relationship of the chemical series was conducted and we found several analogues displaying sub-nanomolar Ki values at the EP3 receptor and micromolar activities at the EP1, EP2 and EP4 receptors. The effect of added human serum albumin (HSA) on the binding affinity at the EP3 receptor was also investigated.