Bradykinin receptor

The bradykinin receptor family is a group of G-protein coupled receptors whose principal ligand is the protein bradykinin.

bradykinin receptor B1
Identifiers
SymbolBDKRB1
NCBI gene623
HGNC1029
OMIM600337
RefSeqNM_000710
UniProtP46663
Other data
LocusChr. 14 q32.1-32.2
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StructuresSwiss-model
DomainsInterPro
bradykinin receptor B2
Identifiers
SymbolBDKRB2
NCBI gene624
HGNC1030
OMIM113503
RefSeqNM_000623
UniProtP30411
Other data
LocusChr. 14 q32.1-32.2
Search for
StructuresSwiss-model
DomainsInterPro

There are two Bradykinin receptors: the B1 receptor and the B2 receptor.[1]

B1 receptor
Main article: bradykinin receptor B1

Bradykinin receptor B1 (B1) is a G-protein coupled receptor encoded by the BDKRB1 gene in humans. Its principal ligand is bradykinin, a 9 amino acid peptide generated in pathophysiologic conditions such as inflammation, trauma, burns, shock, and allergy. The B1 receptor is one of two G protein-coupled receptors that have been found which bind bradykinin and mediate responses to these pathophysiologic conditions.

B1 protein is synthesized by 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.

B2 receptor
Main article: bradykinin receptor B2

The B2 receptor is a G protein-coupled receptor, coupled to Gq and Gi. Gq stimulates phospholipase C to increase intracellular free calcium and Gi inhibits adenylate cyclase. Furthermore, the receptor stimulates the mitogen-activated protein kinase pathways. It is ubiquitously and constitutively expressed in healthy tissues.

The B2 receptor forms a complex with angiotensin converting enzyme (ACE), and this is thought to play a role in cross-talk between the renin-angiotensin system (RAS) and the kinin–kallikrein system (KKS). The heptapeptide angiotensin (1-7) also potentiates bradykinin action on B2 receptors.[2]

Icatibant is a second generation B2 receptor antagonist which has undergone limited clinical trials in pain and inflammation. FR 173657 is another orally active non-peptide B2 antagonist that has undergone limited trials as analgesic and antiinflammatory drug.

Kallidin also signals through the B2 receptor.

References
  1. Leeb-Lundberg LM, Marceau F, Müller-Esterl W, Pettibone DJ, Zuraw BL (2005). "International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences". Pharmacol. Rev. 57 (1): 27–77. doi:10.1124/pr.57.1.2. PMID 15734727. S2CID 8579148.
  2. Fernandes L, Fortes ZB, Nigro D, Tostes RC, Santos RA, Catelli De Carvalho MH (2001). "Potentiation of bradykinin by angiotensin-(1-7) on arterioles of spontaneously hypertensive rats studied in vivo". Hypertension. 37 (2 Part 2): 703–9. doi:10.1161/01.hyp.37.2.703. PMID 11230360.
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