Lys- [Des-Arg9] Bradykinin

Names

[ Name ]:
Lys- [Des-Arg9] Bradykinin

[Synonym ]:
lysyl-des-arg9-bradykinin
h-lys-arg-pro-pro-gly-phe-ser-pro-phe-oh
lys-arg-pro-pro-gly-phe-ser-pro-phe
MFCD00079826
Lys-[Des-Arg9]-Bradykinin

Biological Activity

[Description]:

Lys-[Des-Arg9]Bradykinin, a naturally occurring kinin, is a potent and highly selective bradykinin B1 receptor agonist with a Ki of 0.12 nM, 1.7 nM and 0.23 nM for human, mouse and rabbit B1 receptors, respectively. Lys-[Des-Arg9]Bradykinin has low inhibitory activity on B2 receptors[1][2].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Research Areas >> Metabolic Disease

Signaling Pathways >> GPCR/G Protein >> Bradykinin Receptor

[In Vitro]

Lys-[Des-Arg9]Bradykinin 由缓激肽的蛋白水解裂解形成，通过缓激肽 B1 受体 (B1R) 发挥作用[1]。 Lys-[Des-Arg9]Bradykinin (Lda-BK; 10 μM) 增强 IL-12p70 的分泌并抑制成熟 hMo-DC 的 IL-12p40 分泌。用 Lys-[Des-Arg9]Bradykinin 预处理可减少成熟 hMo-DC 单独向培养基的迁移，表明 Lys-[Des-Arg9]Bradykinin 可抑制成熟 hMo-DC 的趋化作用[1]。

[In Vivo]

Lys-[Des-Arg9]Bradykinin (1 μg；鼻腔注射；新西兰大白兔) 处理可降低脂多糖诱导家兔外周血管阻力，但效果短暂(T1/2=118-195 s)[3]。

[References]

[1]. Rosalind Gulliver, et al. Lys-des[Arg9]-bradykinin alters migration and production of interleukin-12 in monocyte-derived dendritic cells. Am J Respir Cell Mol Biol. 2011 Sep;45(3):542-9.

[2]. L M Fredrik Leeb-Lundberg, et al. International union of pharmacology. XLV. Classification of the kinin receptor family: from molecular mechanisms to pathophysiological consequences. Pharmacol Rev. 2005 Mar;57(1):27-77.

[3]. G Drapeau, et al. Hypotensive effects of Lys-des-Arg9-bradykinin and metabolically protected agonists of B1 receptors for kinins. J Pharmacol Exp Ther. 1991 Dec;259(3):997-1003.

Chemical & Physical Properties

[ Density]:
1.45g/cm3

[ Molecular Formula ]:
C₅₀H₇₃N₁₃O₁₁

[ Molecular Weight ]:
1032.20

[ Exact Mass ]:
1031.56000

[ PSA ]:
377.90000

[ LogP ]:
1.65640

[ Index of Refraction ]:
1.678

[ Storage condition ]:
−20°C

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Articles

Potentiation of des-Arg9-kallidin-induced vasoconstrictor responses by metallopeptidase inhibition in isolated human umbilical artery.

J. Pharmacol. Exp. Ther. 313(3) , 1355-60, (2005)

Several metallopeptidases have been reported to be involved in bradykinin (BK) B(1) receptor agonist metabolism. Our goal was to evaluate in vitro roles of metallopeptidases [e.g., neutral endopeptida...

Kinins and neuroinflammation: dual effect on prostaglandin synthesis.

Eur. J. Pharmacol. 546(1-3) , 197-200, (2006)

The role of kinins, well known as peripheral inflammatory mediators, in the modulation of brain inflammation is unclear. The present data show that bradykinin, a bradykinin B(2) receptor agonist, enha...

Essential role of TM V and VI for binding the C-terminal sequences of Des-Arg-kinins.

Int. Immunopharmacol. 8(2) , 282-8, (2008)

In the kallikrein-kinin and renin-angiotensin systems the main receptors, B1 and B2 (kinin receptors) and AT1 and AT2 (angiotensin receptors) respectively, are seven-transmembrane domain G-protein-cou...