Product Details
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90779-69-4 Name |
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Name |
Atosiban |
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Synonym |
RW-22164;RW-22164;RWJ-22164;Atosiban Impurtiy;atosiban price;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;ATOSIBAN ACETATE |
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90779-69-4 Biological Activity |
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Description |
Atosiban(RW22164; Tractocile) is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane.IC50 value:Target: As a result, there is reduced release of intracellular, stored calcium from the sarcoplasmic reticulum of myometrial cells, and reduced influx of Ca2+ from the extracellular space through voltage gated channels. In addition, atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua.[1][2] In human pre-term labour, atosiban, at the recommended dosage, antagonises uterine contractions and induces uterine quiescence. The onset of uterus relaxation following atosiban is rapid, uterine contractions being significantly reduced within 10 minutes to achieve stable uterine quiescence. |
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Related Catalog |
Signaling Pathways >> GPCR/G Protein >> Oxytocin Receptor Research Areas >> Others |
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References |
[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. |
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90779-69-4 Chemical & Physical Properties |
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Melting point |
>165 °C (dec.) |
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Boiling point |
1469.0±65.0 °C at 760 mmHg |
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Density |
1.3±0.1 g/cm3 |
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Molecular Formula |
C43H67N11O12S2 |
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Molecular Weight |
994.189 |
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Flash Point |
842.2±34.3 °C |
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PSA |
416.27000 |
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LogP |
-3.41 |
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Exact Mass |
993.441223 |
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Vapour Pressure |
0.0±0.3 mmHg at 25°C |
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Index of Refraction |
1.549 |
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Storage condition |
−20°C |
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Water Solubility |
H2O: ≤100 mg/mL |
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90779-69-4 Description |
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Atosiban was introduced in the UK as an injectable inhibitor of preterm labor, a major cause of infant morbidity and mortality. This peptidic oxytocin analog is an antagonist of the vasopressin V1a receptor and of the oxytocin receptor which is found in dramatically increased concentration in the uterine myometrium of pregnant women near term. It competitively inhibited contractions in the pregnant guinea pig uterus induced by oxytocin and vasopressin. In a multicenter, double-blind, placebo-controlled trial, treatment with atosiban caused pregnancy prolongation for up to 7 days in women with more than 28 weeks of gestation. In a comparative clinical trial, atosiban showed a comparable tocolytic action (uterine relaxant) to ritodrine but the former was significantly better tolerated, especially with regards to maternal cardiovascular side effects. In healthy volunteers, plasma levels of atosiban decreased bi-exponentially with an initial and a terminal half-life of 21 min and 1.7h respectively. |
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90779-69-4 Uses |
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Atosiban has been used: as an oxytocin receptor antagonist in the calcium mobilization assay for Z factor determination in uterine myometrium (UT-myo cells) and as a therapeutic agent to inhibit preterm labor to inhibit the activation of oxytocin-receptor-expressing neurons in the parabrachial nucleus of mice (OxtrPBN) |
