A bradykinin B1 receptor antagonist
货号:ajcx26748
CAS:N/A
分子式:C47H75N13O11 • XCF3COOH
分子量：998.2
溶解度:DMF: 1 mg/ml,DMSO: 3 mg/ml,PBS (pH 7.2): 10 mg/ml
纯度：98%
存储：Store at -20°C
库存：现货

Background:

Lys-(Des-Arg⁹, Leu⁸)-Bradykinin is a bradykinin B₁receptor antagonist (K_i= 0.43 nM for the rabbit aorta receptor).¹It is selective for the bradykinin B₁over the B₂receptor (K_i= >10 µM for the rabbit ileum receptor).²Lys-(Des-Arg⁹, Leu⁸)-Bradykinin inhibits contractions induced by the bradykinin B₁receptor agonist Des-Arg⁹-bradykinin in isolated rabbit aortic rings (pA₂= 8.54).³Intraperitoneal 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)