The bradykinin B1 receptor is an inducible G-protein-coupled receptor. It is induced or upregulated at the site of inflammation or injury. A large body of preclinical data supports the development of B1 antagonists as novel therapeutics for the treatment of pain and inflammation. The necessary in vitro and in vivo drug discovery tools are currently available to evaluate novel B1 antagonists. Two major classes of small-molecule B1 antagonists, arylsulfonamide-based and biphenyl-based B1 antagonists, have been disclosed in the last few years.