赖氨酸-(脱-精氨酸9)舒爱激肽

赖氨酸-(脱-精氨酸9)舒爱激肽用途

Lys-[Des-Arg9]缓激肽是一种天然存在的激肽,是一种强效且高选择性的缓激肽B1受体激动剂,对人、小鼠和兔B1受体的Ki分别为0.12 nM、1.7 nM和0.23 nM。Lys-[Des-Arg9]缓激肽对B2受体的抑制活性较低[1][2]。

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赖氨酸-(脱-精氨酸9)舒爱激肽名称

[ CAS 号 ]:
71800-36-7

[ 中文名 ]:
赖氨酸-(脱-精氨酸9)舒爱激肽

[ 英文名 ]:
Lys- [Des-Arg9] Bradykinin

[英文别名 ]:

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

赖氨酸-(脱-精氨酸9)舒爱激肽生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 炎症/免疫

研究领域 >> 代谢疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 缓激肽受体

[体外研究]

赖氨酸-Des-Arg9]缓激肽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] 赖氨酸-[Des-Arg9]缓激肽(Lda BK；10μM)增强白细胞介素-12p70的分泌并抑制成熟 hMo直流电的白细胞介素-12p40分泌。用赖氨酸-Des-Arg9]缓激肽预处理可减少成熟 hMo直流电单独向培养基的迁移,表明赖氨酸-Des-Arg9]缓激肽可抑制成熟 hMo直流电的趋化作用[1]

[体内研究]

赖氨酸-Des-Arg9]缓激肽(1μg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秒)[3]

[参考文献]

[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.

赖氨酸-(脱-精氨酸9)舒爱激肽物理化学性质

[ 密度 ]:
1.45g/cm3

[ 分子式 ]:
C₅₀H₇₃N₁₃O₁₁

[ 分子量 ]:
1032.20

[ 精确质量 ]:
1031.56000

[ PSA ]:
377.90000

[ LogP ]:
1.65640

[ 折射率 ]:
1.678

[ 储存条件 ]:
−20°C

赖氨酸-(脱-精氨酸9)舒爱激肽安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

赖氨酸-(脱-精氨酸9)舒爱激肽文献

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...

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