(Des-Arg)-Bradykinin is an active metabolite of the endogenous vasodilator bradykinin and a peptide agonist of the bradykinin B receptor. It binds to bradykinin B and B receptors (Ks = 1.93 and 8.1 µM, respectively). (Des-Arg)-Bradykinin is formed via carboxypeptidase-mediated cleavage of the bradykinin C-terminal arginine residue in plasma and tissues. It induces relaxation of precontracted isolated endothelium-denuded dog renal artery strips (pD = 8.6). (Des-Arg)-Bradykinin decreases blood pressure in LPS-treated rabbits in a dose-dependent manner.
[Des-Arg9]-Bradykinin is a Bradykinin (B1) receptor agonist that displays selectivity for B1 over B2 receptors.
IC50&Target
Bradykinin B1 Receptor (B1R)
体外研究
The B2 receptor mediates the action of bradykinin (BK) and lysyl-bradykinin (Lys-BK), the first set of bioactive kinins formed in response to injury from kininogen precursors through the actions of plasma and tissue kallikreins, whereas the B1 receptor mediates the action of [Des-Arg9]-Bradykinin (des-Arg9-BK) and Lys-des-Arg Arg9-BK, the second set of bioactive kinins formed through the actions of carboxypeptidases on BK and Lys-BK, respectively.
分子式
C44H61N11O10
分子量
904.02
CAS号
15958-92-6
中文名称
[Des-Arg9]-缓激肽
运输条件
Room temperature in continental US; may vary elsewhere.