KININ B-1 RECEPTORS - A REVIEW

The kinin B-1 receptor has been initially defined as the one mediating the contractile effect of bradykinin (BK)-related peptides in the isolated rabbit aorta. The B-1 receptor is selectively sensitive to kinin metabolites without the C-terminal arginine residue, e.g. des-Arg(9)-BK and Lys-des-Arg(9)-BK; it is apparently rapidly up-regulated in immunopathology under the influence of cytokines and is further regulated by growth factors. Progress in the understanding of this pharmacologic entity is reviewed, including the development of B-1 receptor agonists and antagonists, binding assays, physiopathological applications and the recent cloning and sequencing of the receptor cDNA.