Target intelligence / Profile preview

B2 bradykinin receptor (BDKRB2) (BDKRB2)

Target
BDKRB2
Molecular classification
G protein-coupled receptor, Rhodopsin-like receptor, Receptor
01

Overview

The B2 bradykinin receptor (B2R) is a G protein-coupled receptor (GPCR) that is constitutively expressed in various tissues, including vascular endothelium and smooth muscle [1, 6]. In rabbits, as in humans, it serves as the primary mediator for the physiological actions of bradykinin, a potent vasodilator and inflammatory mediator [2, 3]. Activation of the B2R leads to increased vascular permeability, vasodilation, and pain, primarily through Gq-mediated signaling and calcium mobilization [1, 10]. It plays a critical role in the pathophysiology of hereditary angioedema (HAE), where excessive bradykinin production leads to life-threatening swelling [1, 8]. Therapeutic strategies often focus on B2R antagonism to treat acute HAE attacks and other inflammatory conditions [4, 5]. Rabbit models are frequently used in pharmacological studies because the rabbit B2R shows high sequence homology and similar pharmacological profiles to the human receptor [3, 10].

Other names
B2RBK-2 receptorBradykinin receptor B2BDKRB2
02

Mechanism of action

Antagonism of the B2 bradykinin receptor to inhibit the pro-inflammatory and vasodilatory effects of bradykinin.

03

Biological functions

Signal transductionVasodilationFluid and electrolyte transportSmooth muscle contractionImmune response
04

Disease associations

InflammationHereditary angioedemaCardiovascular diseasePainCancer
05

Safety considerations

HypotensionInjection site reactionsInterference with cardioprotective effects
06

Interacting drugs

Icatibant

5 more in the full profile.

07

Biomarkers

D-dimerVE-cadherin

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