Molecular Classification
G protein-coupled receptor, GPCR
Other Names
Bradykinin receptors, Kinin receptors
Disease Roles
Hereditary angioedemaInflammationChronic pain

Bradykinin Receptor Overview

The bradykinin receptor family comprises G-protein coupled receptors (GPCRs) that mediate the biological effects of bradykinin. The two main subtypes are the Bradykinin receptor B1 (B1R) and Bradykinin receptor B2 (B2R). These receptors play key roles in inflammation, pain, and cardiovascular regulation. B2R is constitutively expressed and mediates normal physiological responses, while B1R is inducible upon tissue injury or inflammation and contributes to chronic pain and inflammation.

Mechanism of Action

Activation of G proteins (Gq, Gi) leading to downstream signaling cascades, including phospholipase C activation and increased intracellular calcium, and inhibition of adenylate cyclase.

Biological Functions

Signal transduction
Vasodilation
Increased vascular permeability
Pain signaling
Inflammation

Disease Associations

Hereditary angioedema
Inflammation
Chronic pain
Cardiovascular disease

Safety Considerations

  • ACE inhibitor-induced cough and angioedema
  • Dysregulation can contribute to hereditary angioedema.

Interacting Drugs

Icatibant
Bradykinin
Kallidin