Target intelligence / Profile preview

Bradykinin Receptor (BRKR)

Target
BRKR
Molecular classification
G protein-coupled receptor, GPCR
01

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.

Other names
Bradykinin receptorsKinin receptors
02

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.

03

Biological functions

Signal transductionVasodilationIncreased vascular permeabilityPain signalingInflammation
04

Disease associations

Hereditary angioedemaInflammationChronic painCardiovascular disease
05

Safety considerations

ACE inhibitor-induced cough and angioedemaDysregulation can contribute to hereditary angioedema.
06

Interacting drugs

Icatibant

2 more in the full profile.

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