Bradykinin receptor B1 (B
1) is a
G-protein coupled receptor
G protein-coupled receptors (GPCRs), also known as seven-(pass)-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptors, and G protein-linked receptors (GPLR), form a large group of protein family, evolution ...
encoded by the BDKRB1
gene
In biology, the word gene (from , ; "...Wilhelm Johannsen coined the word gene to describe the Mendelian units of heredity..." meaning ''generation'' or ''birth'' or ''gender'') can have several different meanings. The Mendelian gene is a ba ...
in humans. Its principal
ligand
In coordination chemistry, a ligand is an ion or molecule (functional group) that binds to a central metal atom to form a coordination complex. The bonding with the metal generally involves formal donation of one or more of the ligand's electr ...
is
bradykinin
Bradykinin (BK) (Greek brady-, slow; -kinin, kīn(eîn) to move) is a peptide that promotes inflammation. It causes arterioles to dilate (enlarge) via the release of prostacyclin, nitric oxide, and endothelium-derived hyperpolarizing factor and ...
, a 9
amino acid
Amino acids are organic compounds that contain both amino and carboxylic acid functional groups. Although hundreds of amino acids exist in nature, by far the most important are the alpha-amino acids, which comprise proteins. Only 22 alpha am ...
peptide generated in pathophysiologic conditions such as inflammation, trauma, burns, shock, and allergy. The B
1 receptor is one of two of G protein-coupled receptors that have been found which bind
bradykinin
Bradykinin (BK) (Greek brady-, slow; -kinin, kīn(eîn) to move) is a peptide that promotes inflammation. It causes arterioles to dilate (enlarge) via the release of prostacyclin, nitric oxide, and endothelium-derived hyperpolarizing factor and ...
and mediate responses to these pathophysiologic conditions.
B
1 protein 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.
Classical agonist of this receptor includes bradykinin1-8 (bradykinin with the first 8 amino acid) and antagonist includes
eu8bradykinin1-8.
Antagonists
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LF22-0542
Safotibant (INN) also known by the research code LF22-0542 is a non-peptide bradykinin B1 antagonist. It displayed binding Ki values of 0.35 and 6.5 nM at cloned human and mouse B1 receptors, respectively, while having no affinity for either huma ...
See also
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Bradykinin receptor
The bradykinin receptor family is a group of G-protein coupled receptors whose principal ligand is the protein bradykinin.
There are two Bradykinin receptors: the B1 receptor and the B2 receptor.
B1 receptor
Bradykinin receptor B1 (B1) is a ...
References
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G protein-coupled receptors
{{transmembranereceptor-stub