Bradykinin receptor B2 (BDKRB2) (BDKRB2)

The Bradykinin receptor B2 (BDKRB2) is a G protein-coupled receptor that serves as a principal mediator of the physiological and pathological effects of bradykinin (UniProt P30551). It is constitutively expressed in various tissues, including the vascular endothelium, where its activation leads to potent vasodilation and increased vascular permeability through the release of nitric oxide and prostacyclin (PubMed PMID: 15607313). In the context of disease, the B2 receptor is a critical target in hereditary angioedema (HAE), as excessive bradykinin generation leads to life-threatening episodes of swelling (StatPearls, Hereditary Angioedema). Pharmacological intervention often involves the use of B2 receptor antagonists, such as icatibant, which competitively inhibit the receptor to treat acute HAE attacks (PubChem CID: 6918173). Additionally, the receptor's activity is indirectly modulated by Angiotensin-Converting Enzyme (ACE) inhibitors, which increase local bradykinin levels by preventing its breakdown (PubMed PMID: 11588345). This accumulation contributes to the antihypertensive efficacy of these drugs but can also lead to side effects like dry cough and angioedema.

Other names

B2RBK-2 receptorB2 bradykinin receptorBradykinin B2 receptorBDKRB2

Competitive antagonism of the B2 receptor to block bradykinin-mediated effects; or indirect activation via the inhibition of bradykinin degradation by ACE inhibitors.