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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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 Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Bradykinin	B1	human	HEK293T	C1198a	DC1198a	MC1198a
	B1	mouse	HEK293T	Cm1198	DCm1198	MCm1198
	B2	human	HEK293T	H1199	DH1199	MH1199
	B2	mouse	HEK293T	Cm1199	DCm1199	MCm1199
	B2	rat	HEK293T	Cr1199	DCr1199	MCr1199
	B2	dog	HEK293T	cd1199	DCd1199	MCd1199
	B2	rhesus monkey	HEK293T	Cpr1199	DCpr1199	MCpr1199
	B2	guinea pig	HEK293T	Cc1199	DCc1199	MCc1199
	B2	rabbit	HEK293T	Cb1199	DCb1199	MCb1199