Bradykinin receptor B1 (IPR001186)
Short name: Brdyknn_1_rcpt
Overlapping homologous superfamilies
Bradykinins are a family of short, structurally similar peptides that activate sensory fibres, contract venous smooth muscle, stimulate release of cytokines, induce connective tissue proliferation and mediate endothelium-dependent vasodilation [PMID: 10812256, PMID: 12755382]. Bradykinin antagonists are used in the treatment of inflammation, asthma, mild pain and endotoxic shock.
Bradykinin receptors are members of the seven transmembrane, rhodopsin-like G-protein coupled receptor family and are widespread in peripheral tissues. There are two bradykinins receptor subtypes: B1 and B2. It has also been proposed there could be further subtypes of the bradykinin receptor, including a tracheal B3 receptor but these, as yet have not been confirmed [PMID: 9112069, PMID: 9650825, PMID: 8075864].
This entry represents bradykinin receptor B1, which has limited distribution in the periphery, and has not been described in the CNS, unlike the bradykinin receptor B2, which is the predominant subtype. Both B1 and B2 receptors are involved in the induction and maintenance of cytokine-induced hyperalgesia. However B1 receptors appear to play a more important role in the development of mechanical hyperalgesia [PMID: 8846417]. The B1 receptor is synthesized de novo following tissue injury and receptor binding leads to an increase in the cytosolic calcium ion concentration, ultimately resulting in chronic and acute inflammatory responses [PMID: 17327486]. In the majority of tissues, bradykinin induces activation of phosphoinositide metabolism via a pertussis-toxin-insensitive G-protein of the Gq/G11 class. It has also been reported to inhibit adenylyl cyclase and raises levels of cyclic guanosine monophosphate (cGMP) and open ion channels. B1 receptor also stimulates phospholipase A2 (PLA2) [PMID: 7700250, PMID: 18725957, PMID: 1695472, PMID: 10614988, PMID: 20152050,PMID: 8832074].
GO:0004947 bradykinin receptor activity
GO:0016021 integral component of membrane
- PR00993 (BRADYKINNB1R)