Abstract
This chapter focuses on bradykinin-1 receptor antagonists. The bradykinin receptor B1 and B2 subtypes are G-protein coupled receptors that are encoded by adjacent genes, BDKRB1 and BDKRB2, on human chromosome 14. The bradykinin receptor subtypes are not highly related and are only slightly more similar to each other than to angiotensin receptors. BK and kallidin are equipotent in activating the bradykinin receptor B2 subtype, whereas DABK and DAK are inactive on this receptor. DABK and DAK activate the bradykinin B1 receptor, with BK and kallidin being less potent. Targeted disruption of the genes encoding the bradykinin B1 and B2 receptors in mice indicate that they are the only receptor subtypes that mediate the biological activity of kinin peptides. Species differences with respect to kinin peptides are apparent for the bradykinin B1 receptor as the affinity for the desArgkinin peptides differs significantly across species. The chapter discusses the role of bradykinin B1 receptors in pain and discusses peptide bradykinin B1 receptor antagonists and nonpeptide bradykinin B1 receptor antagonists.
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