The kinin B1 receptor has been initially defined as the one mediating the contractile effect of bradykinin (BK)-related peptides in the isolated rabbit aorta. The B1 receptor is selectively sensitive to kinin metabolites without the C-terminal arginine residue, e.g. des-Arg9-BK and Lys-des-Arg9-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 B1 receptor agonists and antagonists, binding assays, physiopathological applications and the recent cloning and sequencing of the receptor cDNA.