Key result
The B2-bradykinin receptor exhibits a dual role in physiopathology, offering potential therapeutic targets with agonists for cardiovascular protection and antagonists for inflammation and pain.
This review highlights the dual physiological roles of the B2-bradykinin receptor and suggests that direct targeting with agonists or antagonists could offer therapeutic benefits in cardiovascular and inflammatory diseases.
May guide selective B2-receptor ligand development; extends dual-role concept but leaves open clinical translation.
INTRODUCTION: Kinins are main active mediators of the kallikrein-kinin system (KKS) via bradykinin type 1 inducible (B1R) and type 2 constitutive (B2R) receptors. B2R mediates most physiological bradykinin (BK) responses, including vasodilation, natriuresis, NO, prostaglandins release. AREAS COVERED: The article summarizes knowledge on kinins, B2R signaling and biological functions; highlights crosstalks between B2R and renin-angiotensin system (RAS). The double role (Janus face) in physiopathology, namely the beneficial protection of the endothelium, which forms the basis for the therapeutical utilization of B2 receptor agonists, on the one side, and the involvement of B2R in inflammation or infection diseases and in pain mechanisms, which justifies the use of B2R antagonists, on the other side, is extensively analyzed. EXPERT OPINION: For decades, the B2R has been unconsciously activated during angiotensin-converting enzyme inhibitor (ACEI) or angiotensin receptor blocker (ARB) treatments. Whether direct B2R targeting with stable agonists could bring additional therapeutic benefit to RAS inhibition should be investigated. Efficacy, established in experimental models, should be confirmed by translational studies in cardiovascular pathologies, glaucoma, Duchenne cardiopathy and during brain cancer therapy. The other face of B2R is targeted by antagonists already approved to treat hereditary angioedema. The use of antagonists could be extended to other angioedema and efficacy tested against acute pain and inflammatory diseases.
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Blaes et al. (2013) conducted a review in Cardiovascular pathologies, inflammation, pain, hereditary angioedema. B2 receptor agonists and antagonists was evaluated. The B2-bradykinin receptor exhibits a dual role in physiopathology, offering potential therapeutic targets with agonists for cardiovascular protection and antagonists for inflammation and pain.
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