Lys-(Des-Arg9, Leu8)-Bradykinin is a bradykinin B1 receptor antagonist (Ki = 0.43 nM for the rabbit aorta receptor).1 It is selective for the bradykinin B1 over the B2 receptor (Ki = >10 µM for the rabbit ileum receptor).2 Lys-(Des-Arg9, Leu8)-Bradykinin inhibits contractions induced by the bradykinin B1 receptor agonist Des-Arg9-bradykinin in isolated rabbit aortic rings (pA2 = 8.54).3 Intraperitoneal administration of Lys-(Des-Arg9, Leu8)-bradykinin (5 mg/kg per day for three days) reduces increases in paw edema in a rat model of arthritis induced by peptidoglycan-polysaccharide (PGPS).4
1.MacNeil, T., Bierilo, K.K., Menke, J.G., et al.Cloning and pharmacological characterization of a rabbit bradykinin B1 receptorBiochim. Biophys. Acta1264(2)223-228(1995) 2.Meini, S., Cucchi, P., Catalani, C., et al.Radioligand binding characterization of the bradykinin B2 receptor in the rabbit and pig ileal smooth muscleEur. J. Pharmacol.635(1-3)34-39(2010) 3.Drapeau, G., Audet, R., Levesque, L., et al.Development and in vivo evaluation of metabolically resistant antagonists of B1 receptors for kininsJ. Pharmacol. Exp. Ther.266(1)192-199(1993) 4.Blais, C., Jr., Couture, R., Drapeau, G., et al.Involvement of endogenous kinins in the pathogenesis of peptidoglycan-induced arthritis in the Lewis ratArthritis Rheum.40(7)1327-1333(1997)