Lys-(Des-Arg9)-Bradykinin is a naturally occurring peptide agonist of the bradykinin B1 receptor (Ki = 0.12 nM in HEK293 cells expressing the human receptor).1,2 It is selective for bradykinin B1 over B2 receptors (IC50 = >30,000 nM in CHO cells expressing the human receptor).3 Lys-(Des-Arg9)-Bradykinin increases both mRNA and protein levels of the B1 receptor in IMR-90 human lung fibroblasts in a concentration-dependent manner.4 It induces contraction of isolated rabbit aorta (pD2 = 8.6).5 Lys-(Des-Arg9)-Bradykinin decreases blood pressure in LPS-treated rabbits in a dose-dependent manner.2
1.Bastian, S., Loillier, B., Paquet, J.L., et al.Stable expression of human kinin B1 receptor in 293 cells: Pharmacological and functional characterizationBr. J. Pharmacol.122(2)393-399(1997) 2.Drapeau, G., deBlois, D., and Marceau, F.Hypotensive effects of Lys-des-Arg9-bradykinin and metabolically protected agonists of B1 receptors for kininsJ. Pharmacol. Exp. Ther.259(3)997-1003(1991) 3.Hess, J.F., Borkowski, J.A., Macneil, T., et al.Differential pharmacology of cloned human and mouse B2 bradykinin receptorsMol. Pharmacol.45(1)1-8(1994) 4.Schanstra, J.P., BataillÉ, E., Marin CastaÑo, M.E., et al.The B1-agonist [des-Arg10]-kallidin activates transcription factor NF-kappaB and induces homologous upregulation of the bradykinin B1-receptor in cultured human lung fibroblastsJ. Clin. Invest.101(10)2080-2091(1998) 5.Rhaleb, N.E., Drapeau, G., Dion, S., et al.Structure-activity studies on bradykinin and related peptides: AgonistsBr. J. Pharmacol.99(3)445-448(1990)