Bradykinin receptor (BDKRB) (BDKRB)

Bradykinin is a potent vasoactive nonapeptide generated from high-molecular-weight kininogen by the action of plasma kallikrein (StatPearls, PMID: 30725873). It exerts its biological effects through two distinct G protein-coupled receptors: the B1 receptor (BDKRB1) and the B2 receptor (BDKRB2) (UniProt, P30551, P30552). The B2 receptor is constitutively expressed in most tissues and mediates the primary physiological roles of bradykinin, such as vasodilation, increased vascular permeability, and smooth muscle contraction (IUPHAR/BPS Guide to Pharmacology). In contrast, the B1 receptor is typically induced following tissue injury or in response to pro-inflammatory cytokines like interleukin-1 (UniProt, P30551). Dysregulation of the bradykinin system, particularly overproduction or impaired degradation, is a hallmark of hereditary angioedema (HAE), leading to life-threatening episodes of localized swelling (NIH, GARD). Therapeutic strategies include the use of B2 receptor antagonists like icatibant to block the effects of excess bradykinin or kallikrein inhibitors like lanadelumab to prevent its formation (PubChem, CID 6918173). Beyond HAE, the bradykinin system is a target of interest in treating inflammation, chronic pain, and cardiovascular diseases such as hypertension (StatPearls, PMID: 30725873).

Other names

B1 receptorB2 receptorBDKRB1BDKRB2Kinin receptorBK receptorB1RB2R

Antagonism of the B2 receptor to block bradykinin-induced vasodilation and edema; inhibition of plasma kallikrein to reduce the synthesis of bradykinin from kininogen (PubChem, CID 6918173; StatPearls, PMID: 30725873).