90779-69-4
90779-69-4 结构式
基本信息
阿托西班
1-deamino-2d-tyr-(oet)-4-thr-8-orn-oxytocin
oxytocin,1-(3-mercaptopropanoicacid)-2-(o-ethyl-d-tyrosine)-4-l-threonine-8-l
rwj22164
1-(3-Mercaptopropionic acid)-2-(3-(p-ethoxyphenyl)-D-alanine)-4-L-thre onine-8-L-ornithineoxytocin
[Mpr-D-Tyr(OEt)-Ile-Thr-Asn-Cys]-Pro-Orn-Gly-NH2
(2S)-N-[(1S)-4-Amino-1-(carbamoylmethylcarbamoyl)butyl]-1-[(4S,7S,13S,16R)-13-[(2S)-butan-2-yl]-7-(carbamoylmethyl)-16-[(4-ethoxyphenyl)methyl]-10-(1-hydroxyethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carbonyl]pyrrolidine-2-carboxamide
1-(3-Mercaptopropanoic acid)-2-(O-ethyl-D-tyrosine)-4-L-threonine-8-L-ornithineoxytocin
1-Deamino-2-D-Tyr-(O-ethyl)-4-Thr-8-ornoxytocin
Atosiban
Human Atosiban
1-Deamino-2-D-Tyr-(O-ethyl)-4-Thr-8-ornoxytocin, Tractocile, 1-(3-Mercaptopropanoic acid)-2-(O-ethyl-D-tyrosine)-4-L-threonine-8-L-ornithineoxytocin
物理化学性质
常见问题列表
醋酸阿托西班是由9个氨基酸组成的二硫键型的环状多肽，是1，2，4和8位修饰的缩宫素分子，肽的N端为3-巯基丙酸(巯基与[Cys]6的巯基形成二硫键)，C端为酰胺的形式，N端第二氨基酸是乙基化修饰的[D-Tyr(Et)]2，醋酸阿托西班在药品中以醋酸盐的形式存在，通用名为醋酸阿托西班。
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.
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.