Bradykinin receptors are cell surface, G-protein coupled receptors of the seven-transmembrane domain family. The existence of two subtypes of bradykinin receptor, BDKRB1 and BDKRB2, has been confirmed through the use of high-affinity peptide and nonpeptide receptor antagonists, radioligand binding studies, receptor cloning and expression studies. The principal ligand of bradykinin receptors is bradykinin, a 9 amino acid peptide, which acts through the receptors to elicit a series of biological responses. BDKRB2 receptors are ubiquitously and constitutively expressed in healthy tissues and are most commonly found in various vascular and non-vascular smooth muscles, while BDKRB1 receptors are formed in vitro during trauma and injury, and are found in bone tissues.
BDKRB2 receptors mediate a variety of physiological processes, including bronchoconstriction, local blood flow regulation, hypotension, acute inflammatory reactions, pain, and hyperalgesia. BDKRB1 receptors are involved in pathophysiologic conditions such as inflammation, trauma, burns, shock, and allergy. They have been implicated in processes such as hyperalgesia, plasma extravasation, white blood cell activation, and accumulation, and blood pressure regulation.
Numerous bradykinin receptor antagonists have been synthesized to treat different diseases, such as rheumatoid arthritis, inflammatory bowel disease, asthma, rhinitis, sore throat, allergic reactions, pain, inflammatory skin disorders, hypertension, etc. Due to their important role in different disease states, bradykinin receptors have been actively studied in terms of their structure, biological functions, and applications. Here, we give an introduction to the two subtypes of this receptor family.
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