Bradykinin GPCR Family Subtypes and Products

What Are Bradykinin Receptors?

Bradykinin receptors are a family of G protein-coupled receptors (GPCRs) consisting of 2 receptors: B1 and B2. The principal ligand, bradykinin is present during conditions such as burns, trauma, allergies, shock, and inflammation. When bound with B1, an acute or chronic inflammatory response is exhibited. B2 antagonist Icatibant has already been approved in the United States and Europe for the treatment of angioedema, and limited trials have been done to assess the validity of Icatibant as an analgesic and anti-inflammatory medication.

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Bradykinin Receptor Information

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B1

B2

Bradykinin B1 is a receptor for bradykinin and mediates responses to pathophysiological conditions such as inflammation, trauma, burns, shock, and allergy. Receptors for B1 are normally absent, but become highly upregulated after inflammatory stimuli. B1 receptor agonists may have important clinical value in the treatment of chronic pain and inflammatory disorders.

Bradykinin B2 receptor agonists may have important clinical value in the treatment and prevention of various cardiovascular disorders such as hypertension, ischemic heart disease, left ventricular hypertrophy, ventricular remodeling and congestive heart failure, as well as diabetic disorders by mimicking the reported beneficial effects of bradykinin. Blocking bradykinin B2 receptors after experimental cerebral ischemia reduces brain edema, infarct volume and neuronal necrosis, and improves neurological outcome. Thus, B2 antagonists may be a promising new class of compounds for clinical use after the onset of cerebral ischemia.

Bradykinin Cell Lines

Receptor FamilyReceptorSpeciesParentalStable Cell Lines Division-Arrested Cells Membranes
BradykininB1humanHEK293TC1198aDC1198aMC1198a
B1mouseHEK293TCm1198DCm1198MCm1198
B2humanHEK293TH1199DH1199MH1199
B2mouseHEK293TCm1199DCm1199MCm1199
B2ratHEK293TCr1199DCr1199MCr1199
B2dogHEK293T cd1199 DCd1199MCd1199
B2rhesus monkeyHEK293TCpr1199DCpr1199MCpr1199
B2guinea pigHEK293TCc1199DCc1199MCc1199
B2rabbitHEK293TCb1199DCb1199MCb1199

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