Lys-(Des-Arg9, Leu8)-Bradykinin (trifluoroacetate salt) (Synonyms: Des-Arg10,Leu9-Kallidin, Des-Arg10,Leu9-KD, LysLeu8Des-Arg9-BK, LysLeu8Des-Arg9-Bradykinin)

Lys-(Des-Arg⁹, Leu⁸)-Bradykinin is a bradykinin B₁ receptor antagonist (K_i = 0.43 nM for the rabbit aorta receptor).¹ It is selective for the bradykinin B₁ over the B₂ receptor (K_i = >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)