(hyp³)-bradykinin acetate

(Hyp³)-Bradykinin acetate is an agonist of bradykinin B2 receptor and stimulates inositol phosphate production in cultured human fibroblasts.

Bradykinin (acetate) is an active peptide that is generated by the kallikrein-kinin system. It is a inflammatory mediator and also recognized as a neuromediator and regulator of several vascular and renal functions. Enzymatically produced from kallidin in the blood, it is a powerful vasodilator that causes smooth muscle contraction, and may mediate inflammation. It has a role as a human blood serum metabolite and a vasodilator agent. It is a tautomer of a bradykinin(2+).

Lys-[Des-Arg9]Bradykinin acetate is an endogenous potent and highly selective bradykinin B1 receptor agonist (Ki values are 0.12 and > 30000 nM at human B1 and B2 receptors respectively). Hypotensive agent that reduces peripheral vascular resistance in vivo. 16-fold more potent than [Des-Arg9]-Bradykinin.

Sar-[D-Phe8]-des-Arg9-Bradykinin acetate is a potent and selective bradykinin B1 receptor agonist (EC50 = 9.02 nM in rabbit aorta) that is resistant to aminopeptidase, kininase I and II (ACE) and neutral endopeptidase cleavage. Exhibits hypotensive and angiogenic activity in vivo.

Lys-Bradykinin acetate is an endogenous bradykinin receptor agonist.

[Des-Arg9]-Bradykinin acetate is a selective agonist of the Bradykinin B1 receptor.

Des-Arg9-[Leu8]-Bradykinin acetate is a potent antagonist of the bradykinin receptor 1 (B1R) used in renal fibrosis research [1].