A new class of nonpeptide bradykinin B2 receptor ligand, incorporating a 4-aminoquinoline framework. Identification of a key pharmacophore to determine species …
Introduction of various aliphatic amino groups at the 4-position of the quinoline moiety of our nonpeptide bradykinin (BK) B2 receptor antagonists afforded highly potent ligands for human B2 receptor with various affinities for guinea pig B2 receptor, indicating remarkable species difference. A representative 4-dimethyamino derivative 40a exhibited subnanomolar and nanomolar binding affinities for human and guinea pig B2 receptors, respectively, and ...