Bradykinin is a potent vasodilator peptide that exerts its vasodilatory action through stimulation of specific endothelial B2 receptors, thereby causing the release of prostacyclin, NO, and EDHF.Bradykinin (BK) has been reported to be involved in the progression of many types of cancer. Two bradykinin receptors, bradykinin B1 receptor (B1R) and bradykinin B2 receptor (B2R), are significantly expressed in all the tested colorectal cancer cells. Repression of B2R, but not B1R, attenuates the BK-mediated invasion and migration, and inhibits ERK1/2 activation and IL-6 production. Moreover, blocking of the ERK pathway decreases the BK-mediated IL-6 production. In addition, IL-6 repression suppresses the effects of BK on colorectal cancer cell invasion and migration.Bradykinin, the enzymatic product of kallikrein-kinin system (KKS), is a major modulator of Ang II actions on blood volume, vascular reactivity and salt sensitivity.
||ELN-441958 is a potent, neutral antagonist of B1 receptor, inhibits the binding of the B1 agonist ligand [3H]DAKD to IMR-90 cells with Ki of 0.26 nM. ELN-441958 is highly selective for B1 over B2 receptors, and >500/ 2000-fold selective for the B1 over μ/δ-opioid receptor.
||Bradykinin is a 9-amino acid peptide (Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg).
||A selective and specific antagonist of bradykinin B2 receptor (B2R) with IC50 and Ki of 1.07 nM and 0.798 nM respectively.