BDKRB1

The BDKRB1 gene encodes the bradykinin receptor B1 (B1R), a G-protein coupled receptor (GPCR) with aliases such as BK1R. Normally undetectable in healthy tissues, B1R is rapidly upregulated by inflammation, tissue injury, or microbial infection, binding des-Arg9-bradykinin to mediate pro-inflammatory and nociceptive responses.
B1R activation triggers Gq/11 and Gi/o signaling pathways, leading to intracellular calcium release, nitric oxide production, and MAPK activation. It is implicated in rheumatoid arthritis, neuropathic pain, and cardiovascular disorders. Several B1R antagonists (e.g., SSR240612) are under preclinical or early clinical investigation for pain and inflammation, though no drugs targeting B1R have been approved to date.