9-L-Leucine-1-9-kallidin

Description

Lys-(des-Arg9, Leu8)-Bradykinin trifluoroacetate salt is a peptide chain containing nine amino acids. The amino acid sequence of bradykinin is Arg-Pro-Pro-Gly-Phe-Ser-Pro-Phe-Arg (RPPGFSPFR). Bradykinin is a peptide that causes blood vessels to dilate, thus resulting in lower blood pressure. A class of drugs used to lower blood pressure called ACE inhibitors lower blood pressure by increasing the concentration of bradykinin (by inhibiting its degradation). Bradykinin acts on blood vessels by releasing prostacyclin, nitric oxide, and endothelial-derived hyperpolarizing factors.

Uses

Lys-(Des-Arg9,Leu8)-Bradykinin is a bradykinin B1 receptor antagonist[1].

Application

As one of the end effectors of the kallikrein-kinin system,Lys-(des-Arg9, Leu8)-Bradykinin trifluoroacetate salt has various biological activities, such as vasodilator, increase vascular permeability, induce contraction of non-vascular smooth muscle and so on.

Mechanism of action

Lys-(des-Arg9, Leu8)-Bradykinin trifluoroacetate salt is a potent endothelium-dependent vasodilator that causes non-vascular smooth muscle contraction, increases vascular permeability and is also involved in pain mechanisms. Bradykinin also causes an increase in urine sodium, which helps lower blood pressure.

It increases calcium levels inside neocortical astrocytes, causing them to release glutamate.

In some patients treated with angiotensin I-converting enzyme (ACE) inhibitors, bradykinin has been implicated as a cause of dry cough. This difficult-to-treat cough usually results from discontinuation of ACE inhibitor therapy. In such cases, angiotensin II receptor antagonists are used as the next step in therapy.

References

[1] Gieldon A, et, al. Theoretical study of the human bradykinin-bradykinin B2 receptor complex. Chembiochem. 2008 Oct 13;9(15):2487-97. DOI:10.1002/cbic.200800324
[2] TANYA MACNEIL. Cloning and pharmacological characterization of a rabbit bradykinin B1 receptor[J]. Biochimica et Biophysica Acta (BBA) - Gene Structure and Expression, 1995, 1264 2: Pages 223-228. DOI: 10.1016/0167-4781(95)00152-7
[3] STEFANIA MEINI. Radioligand binding characterization of the bradykinin B2 receptor in the rabbit and pig ileal smooth muscle[J]. European journal of pharmacology, 2010, 635 1: Pages 34-39. DOI: 10.1016/j.ejphar.2010.03.012
[4] G DRAPEAU. Development and in vivo evaluation of metabolically resistant antagonists of B1 receptors for kinins.[J]. Journal of Pharmacology and Experimental Therapeutics, 1993, 266 1: 192-199.
[5] CHARLES BLAIS JR. Involvement of endogenous kinins in the pathogenesis of peptidoglycan-induced arthritis in the Lewis rat[J]. Arthritis & Rheumatology, 2005, 40 7: 1327-1333. DOI: 10.1002/art.1780400718