B2 bradykinin receptor (BDKRB2)

The B2 bradykinin receptor (BDKRB2) is a G protein-coupled receptor that serves as a primary mediator of the physiological and pathological effects of the kallikrein-kinin system (UniProt P30551). It is constitutively expressed in many tissues, including vascular endothelium and smooth muscle, where it responds to the endogenous ligands bradykinin and kallidin (PubMed: 15155814). Activation of the B2 receptor leads to the mobilization of intracellular calcium and the production of nitric oxide, resulting in potent vasodilation and increased vascular permeability (StatPearls: NBK538214). In clinical medicine, the B2 receptor is a critical therapeutic target for hereditary angioedema (HAE), a condition characterized by excessive bradykinin production leading to severe swelling (PubMed: 21722644). Drugs like icatibant act as selective, competitive antagonists at this receptor to terminate acute HAE attacks by blocking bradykinin-induced vascular leakage (PubChem CID: 6918173). Beyond angioedema, the receptor is also implicated in pain signaling and inflammatory responses, making it a focus for research into analgesics and anti-inflammatory therapies.

Other names

BK-2 receptorB2RBradykinin receptor B2BDKR2

Competitive antagonism of the B2 receptor to inhibit the vasodilation and vascular permeability effects of bradykinin.