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Kinins are proinflammatory peptides that mediate numerous vascular and pain responses to tissue injury. Two pharmacologically distinct kinin receptor subtypes have been identified and characterized for these peptides, which are named B₁ and B₂ and belong to the rhodopsin family of G protein-coupled receptors. The B₂ receptor mediates the action of bradykinin (BK) and lysyl-bradykinin (Lys-BK), the first set of bioactive kinins formed in response to injury from kininogen precursors through the actions of plasma and tissue kallikreins, whereas the B₁ receptor mediates the action of des-Arg⁹-BK and Lys-des-Arg⁹-BK, the second set of bioactive kinins formed through the actions of carboxypeptidases on BK and Lys-BK, respectively. The B₂ receptor is ubiquitous and constitutively expressed, whereas the B₁ receptor is expressed at a very low level in healthy tissues but induced following injury by various …