Kinins contribute to the acute inflammatory response and are implicated in the pathophysiology of inflammatory disease. The development of therapeutically viable agents that counteract the effects of kinins is, therefore, potentially very rewarding. Since kinin actions are generally mediated via an interaction with cell-surface receptors, one approach is the development of site-specific receptor antagonists. The emphasis in this review is to outline our current understanding of the properties of bradykinin receptors and the potential therapeutic applications for drugs acting at these sites. As a result of the recent introduction of potent bradykinin receptor antagonists and the cloning of bradykinin receptor genes, considerable advances in kinin research can now be confidently anticipated.