BRADYKININS Dr. Sarita Sharma Associate Professor MMCP, MMDU
BRADYKININS Inflammatory mediator Bradykinin is a 9-amino acid peptide chain . The amino acid sequence of bradykinin is: Arg - Pro - Pro - Gly - Phe - Ser - Pro - Phe - Arg (RPPGFSPFR). Its empirical formula is therefore C 50 H 73 N 15 O 11 . Bradykinin formed by proteolytic cleavage of circulating proteins termed kininogens ( biologocal peptide).
Biosynthesis: The kinin-kallikrein system makes bradykinin by kininogen precursor proteolytic cleavage high-molecular-weight kininogen (HMWK) enzyme kallikrein active ( serine proteases , ) bradykinin Pre- kallikrein inactive Hagemen’s factor (factor XII)
KININS RECEPTORS, ACTIONS & THERAPY Activate β 1 , β 2 , β 3 receptors linked to PLC/A 2 Powerful Vasodilation→ decreased blood pressure via 2 receptor stimulation Increase in capillary permeability inducing edema. Produces inflammation & pain. ( 2 ) Cardiac stimulation: Compensatory indirect & direct tachycardia & increase in cardiac output It produces coronary vasodilation
PHARMACOLOGICAL ACTIONS Vasodilatation Increased vascular permeability Stimulation of epithelial ion transport and fluid secretion in airways and gastrointestinal tract
KININS ACTIONS & THERAPY Kinins produce broncho-constriction & itching in respiratory system Therapeutic Use: No current use of kinin analogues Increased Bradykinin is possibly involved in the therapeutic efficiency & cough produced by ACEIs ACE inhibitors BP & bradykinins