醋酸阿托西班

中文名称:

醋酸阿托西班

中文同义词:

阿托西班醋酸盐;醋酸阿托西班

英文名称:

Atosiban Acetate

英文同义词:

1-{[7-(2-Amino-2-oxoethyl)-13-sec-butyl-16-(4-ethoxybenzyl)-10-(1 -hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pent aazacycloicosan-4-yl]carbonyl}prolylornithylglycinamide acetate ( 1:1);(2S)-N-[(2S)-5-amino-1-[(2-amino-2-oxoethyl)amino]-1-oxopentan-2-yl]-1-[(4R,7S,10S,13S,16R)-7-(2-amino-2-oxoethyl)-13-[(2S)-butan-2-yl]-16-[(4-ethoxyphenyl)methyl]-10-[(1R)-1-hydroxyethyl]-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide;(2S)-N-((S)-5-amino-1-((2-amino-2-oxoethyl)amino)-1-oxopentan-2-yl)-1-((4R,7S,10S,16R)-7-(2-amino-2-oxoethyl)-13-((S)-sec-butyl)-16-(4-ethoxybenzyl)-10-((R)-1-hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentaazacycloicosane-4-carbonyl)pyrrolidine-2-carboxamide acetate;Atosiban acetate (90779-69-4 free base)

CAS号:

914453-95-5

分子式:

C45H71N11O14S2

分子量:

1054.25

EINECS号:

相关类别:

原料药;原料药（API）;多肽中间体;贝尔卡主打;陕西林奈主打产品;Amines, Aromatics, Heterocycles, Pharmaceuticals, Intermediates Fine Chemicals

Mol文件:

914453-95-5.mol

生物活性

Atosiban acetate (RW22164 acetate;RWJ22164 acetate) 是一种九肽，竞争性的加压素/催产素受体 (vasopressin/oxytocin receptor) 拮抗剂，也是一种脱氨基催产素类似物。Atosiban acetate 是一种主要的宫缩抑制剂，可用于自发早产的研究。

体外研究

Atosiban inhibits the oxytocin-mediated release of IP3 from the myometrial cell membrane. There is reduced release of intracellular, stored calcium from the sacroplasmic reticulum of myometrial cells, and reduced influx of Ca 2+ from the extracellular space through voltage gated channels. In addition, Atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua.

体内研究

The posterior pituitary hormones, oxytocin and arginine vasopressin, differ in structure by only two amino acids, and Atosiban influences physiological effects of arginine vasopressin on the feto-maternal cardiovascular and renal systems. In late-gestation sheep, the administration of Atosiban for 1 hour fails to induce fetomaternal cardiovascular changes. Atosiban blocks the activation of oxytocin-receptor-expressing neurons in the parabrachial nucleus of mice.