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阿托西班

阿托西班用途

Atosiban(RW22164; Tractocile)为九肽,是desamino-oxytocin类似物,是竞争性加压素/催产素受体拮抗剂,能抑制催产素介导的三磷酸肌醇从子宫肌层细胞膜上释放。

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阿托西班名称

[ CAS 号 ]:
90779-69-4

[ 中文名 ]:
阿托西班

[ 英文名 ]:
(Deamino-Cys1,D-Tyr(Et)2,Thr4,Orn8)-Oxytocin acetate salt

[英文别名 ]:

1-Deamino-2-D-Tyr-(O-ethyl)-4-Thr-8-ornoxytocin
MFCD00672436
antocin
ATOSIBAN ACETATE
1-deamino-2d-tyr-(oet)-4-thr-8-orn-oxytocin
Tractocile
Atosiban
[Mpr-D-Tyr(OEt)-Ile-Thr-Asn-Cys]-Pro-Orn-Gly-NH2

阿托西班生物活性

[ 描述 ]:

Atosiban(RW22164; Tractocile)为九肽,是desamino-oxytocin类似物,是竞争性加压素/催产素受体拮抗剂,能抑制催产素介导的三磷酸肌醇从子宫肌层细胞膜上释放。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 催产素受体

研究领域 >> 其他

[参考文献]

[1]. Sanu O, et al. Critical appraisal and clinical utility of atosiban in the management of preterm labor. Ther Clin Risk Manag. 2010 Apr 26;6:191-9.

[2]. Akerlund M, et al. The effect on the human uterus of two newly developed competitive inhibitors of oxytocin and vasopressin. Acta Obstet Gynecol Scand. 1985;64(6):499-504.

[相关活性小分子]

阿托西班物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
1469.0±65.0 °C at 760 mmHg

[ 分子式 ]:
C₄₃H₆₇N₁₁O₁₂S₂

[ 分子量 ]:
994.189

[ 闪点 ]:
842.2±34.3 °C

[ 精确质量 ]:
993.441223

[ PSA ]:
416.27000

[ LogP ]:
-3.41

[ 外观性状 ]:
固体

[ 蒸汽压 ]:
0.0±0.3 mmHg at 25°C

[ 折射率 ]:
1.549

[ 储存条件 ]:
−20°C

[ 水溶解性 ]:
H2O: ≤100 mg/mL

阿托西班MSDS

详细MSDS(安全技术说明书)

阿托西班毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RS7590000

CHEMICAL NAME :: Oxytocin, 1-(3-mercaptopropanoic acid)-2-(O-ethyl-D-tyrosine)-4-L-threonine-8-L-ornith ine

CAS REGISTRY NUMBER :: 90779-69-4

LAST UPDATED :: 198912

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C43-H67-N11-O12-S2

MOLECULAR WEIGHT :: 994.33

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

DOSE :: 94 ug/kg

SEX/DURATION :: female 1-35 week(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects

REFERENCE :: BJOGAS British Journal of Obstetrics and Gynaecology. (Blackwell Scientific Pub. Ltd., POB 88, Oxford, UK) V.82- 1975- Volume(issue)/page/year: 94,1040,1987

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阿托西班安全信息

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

[ RTECS号 ]:
RS7590000

阿托西班文献

Reversal of peripheral nerve injury-induced hypersensitivity in the postpartum period: role of spinal oxytocin.

Anesthesiology 118(1) , 152-9, (2013)

Physical injury, including surgery, can result in chronic pain; yet chronic pain following childbirth, including cesarean delivery in women, is rare. The mechanisms involved in this protection by preg...

Development and clinical experience with the new evidence-based tocolytic atosiban.

Acta Obstet. Gynecol. Scand. 81(7) , 633-41, (2002)

The incidence of preterm birth has remained unchanged for the last few decades. This is due, in part, to the complex etiology of preterm labor, and the limited ability of tocolytic agents to prolong p...

Oxytocin regulates changes of extracellular glutamate and GABA levels induced by methamphetamine in the mouse brain.

Addict. Biol. 17(4) , 758-69, (2012)

Oxytocin (OT), a neurohypophyseal neuropeptide, affects adaptive processes of the central nervous system. In the present study, we investigated the effects of OT on extracellular levels of glutamate (...

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