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(D(CH2)51,TYR(ET)2,VAL4,ARG8)-VASOPRESSIN

用途

SKF 100398 (d(CH2)5Tyr(Et)VAVP) 是一种精氨酸加压素 (AVP) 类似物,能作为外源性和内源性 AVP 抗利尿作用的特异性拮抗剂。

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名称

[ CAS 号 ]:
77453-01-1

[ 中文名 ]:
(D(CH2)51,TYR(ET)2,VAL4,ARG8)-VASOPRESSIN

[ 英文名 ]:
SKF 100398

[英文别名 ]:

M.W. 1136.41 C53H77N13O11S2
type 1 arginine vasopressin antagonist
(d(CH2)51,Tyr(Et)2,Val4,Arg8)-Vasopressin

生物活性

[ 描述 ]:

SKF 100398 (d(CH2)5Tyr(Et)VAVP) 是一种精氨酸加压素 (AVP) 类似物,能作为外源性和内源性 AVP 抗利尿作用的特异性拮抗剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 血管加压素受体

研究领域 >> 代谢疾病

[体内研究]

SKF 100398是外源性和内源性AVP通水作用的特异性拮抗剂[1]。SKF 100398(8个)μg/kg；i、消除AVP的抗利尿作用[1]。动物模型：雄性Sprague-Dawley大鼠(250-300g)[1]剂量：8μg/kg给药：静脉注射结果：完全阻断外源性AVP(4ng/kg体重)的抗利尿作用。

[参考文献]

[1]. S Ishikawa, et al. Further in vivo evidence for antagonist-to-antidiuretic action of arginine vasopressin. Am J Physiol. 1983 Nov;245(5 Pt 1):R713-9.

物理化学性质

[ 密度 ]:
1.44g/cm3

[ 分子式 ]:
C₅₃H₇₇N₁₃O₁₁S₂

[ 分子量 ]:
1136.39000

[ 精确质量 ]:
1135.53000

[ PSA ]:
431.92000

[ LogP ]:
4.60970

[ 折射率 ]:
1.676

安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H332

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
20

[ 安全声明 (欧洲) ]:
36

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

合成路线

详细合成路线

文献

Vasopressin increases water permeability of kidney collecting duct by inducing translocation of aquaporin-CD water channels to plasma membrane.

Proc. Natl. Acad. Sci. U. S. A. 92(4) , 1013-7, (1995)

Water excretion by the kidney is regulated by the peptide hormone vasopressin. Vasopressin increases the water permeability of the renal collecting duct cells, allowing more water to be reabsorbed fro...

Arginine vasopressin enhances pHi regulation in the presence of HCO3- by stimulating three acid-base transport systems.

Nature 337(6208) , 648-51, (1989)

Growth factors raise intracellular pH (pHi) by stimulating Na+/H+ exchange in the absence of HCO3-. In mutant cells that lack the Na+/H+ exchange activity, this alkalinization does not occur, and the ...

Pharmacological characterization of V1a vasopressin receptors in the rat cortical collecting duct.

Am. J. Physiol. 262 , F546-F553, (1992)

Vasopressin receptors in distal segments of the rat nephron were identified in isolated tubules using two labeled ligands: the [1-(beta-mercapto-beta,beta-cyclopentamethylenepropionic acid), 2-(O-meth...

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