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艾替班特乙酸盐

艾替班特乙酸盐用途

Icatibant acetate (HOE-140 acetate) 是有效的,特异的缓激肽 B2 受体拮抗剂,IC50 和 Ki 值分别为 1.07 nM和 0.798 nM。

艾替班特乙酸盐名称

[ CAS 号 ]:
138614-30-9

[ 中文名 ]:
艾替班特醋酸盐

[ 英文名 ]:
Icatibant acetate

[中文别名 ]:

艾替班特乙酸盐

[英文别名 ]:

Icatibant acetate

艾替班特乙酸盐生物活性

[ 描述 ]:

Icatibant acetate (HOE-140 acetate) 是有效的,特异的缓激肽 B2 受体拮抗剂,IC50 和 Ki 值分别为 1.07 nM和 0.798 nM。

[ 相关类别 ]:

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 缓激肽受体

[体外研究]

Icatibant(10-30μM)增强血管紧张素III,但不增强血管紧张素II(由血管紧张素AT1受体介导的收缩)和Lys-des-Arg9-缓激肽,但不能增强des-Arg9-缓激肽(缓激肽B1受体介导的作用)[3]。

[体内研究]

Icatibant(10-30μM)增强血管紧张素III,但不增强血管紧张素II(由血管紧张素AT1受体介导的收缩)和Lys-des-Arg9-缓激肽,但不能增强des-Arg9-缓激肽(缓激肽B1受体介导的作用)[3]。动物模型：CBA/J(H-2k)株雌性小鼠[2]。剂量：0.06、0.3或1.5mg/kg。给药：皮下给药,每日两次。结果：1.5mg/kg剂量组大鼠小肠长度为93.6±6.8mm,0.3mg/kg剂量组大肠长度为94.0±4.1mm,对缩短有明显的预防作用。

[参考文献]

[1]. Hock FJ, et al. Hoe 140 a new potent and long acting bradykinin-antagonist: in vitro studies. Br J Pharmacol. 1991 Mar;102(3):769-73.

[2]. Y Arai, et al. Effect of Icatibant, a Bradykinin B2 Receptor Antagonist, on the Development of Experimental Ulcerative Colitis in Mice. Dig Dis Sci. 1999 Apr;44(4):845-51.

[3]. Marie-Thérèse Bawolak, et al The Bradykinin B2 Receptor Antagonist Icatibant (Hoe 140) Blocks Aminopeptidase N at Micromolar Concentrations: Off-Target Alterations of Signaling Mediated by the Bradykinin B1 and Angiotensin Receptors. Eur J Pharmacol. 2006 Dec 3;551(1-3):108-11.

艾替班特乙酸盐物理化学性质

[ 密度 ]:
1.6g/cm3

[ 分子式 ]:
C₆₁H₉₃N₁₉O₁₅S

[ 分子量 ]:
1364.57000

[ 精确质量 ]:
1363.68000

[ PSA ]:
581.76000

[ LogP ]:
1.67610

[ 外观性状 ]:
粉末

[ 储存条件 ]:
-20℃

艾替班特乙酸盐安全信息

[ 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

艾替班特乙酸盐文献

Contribution of endogenous bradykinin to fibrinolysis, inflammation, and blood product transfusion following cardiac surgery: a randomized clinical trial.

Clin. Pharmacol. Ther. 93(4) , 326-34, (2013)

Bradykinin increases during cardiopulmonary bypass (CPB) and stimulates the release of nitric oxide, inflammatory cytokines, and tissue-type plasminogen activator (t-PA), acting through its B2 recepto...

Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells.

Am. J. Physiol. Cell Physiol. 303(12) , C1260-8, (2012)

In this study, the interaction of natriuretic peptides (NP) and bradykinin (BK) signaling pathways was identified by measuring membrane potential (V(m)) and intracellular Ca(2+) using the patch-clamp ...

Influence of kinin peptides on monocyte-endothelial cell adhesion.

J. Cell. Biochem. 115(11) , 1985-95, (2014)

Adhesion of leukocytes to vascular endothelium in response to proinflammatory mediators is an important component of the overall inflammatory reaction. In the current work, we used a retinoic acid-dif...

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