Icatibant acetate (HOE-140 acetate) is a potent and specific peptide antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.

SSR240612 is a potent and selective non-peptide bradykinin B1 receptor antagonist with Kis of 0.48 nM and 0.73 nM for B1 kinin receptors of human fibroblast MRC5 and HEK cells expressing human B1 receptors, 481 nM and 358 nM for B2 receptors of guinea pig ileum membranes and CHO cells expressing human B1 receptor, respectively.

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.

Bradykinin is a pro-inflammatory polypeptide. It is an important mediator of hyperalgesia, inflammatory diseases, asthma and cancer with anti-cancer activities. Targeting the bradykinin system by either blocking the bradykinin production may open a new potential therapeutic window for the treatment of COVID-19 induced acute respiratory distress syndrome (ARDS) particularly before patients enter the irreversible stages.

Bradykinin (1-6), an amino-truncated bradykinin peptide, is stable metabolite of bradykinin cleaved by carboxypeptidase Y (CPY).