Atosiban

SKU: orb1223687

Description

A nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist; inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane; is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Other Indication Approved.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 90779-69-4
• MW: 994.1886
• Purity: >98% (HPLC)
• Formula: C₄₃H₆₇N₁₁O₁₂S₂
• SMILES: CCOc1ccc(C[C@H]2NC(CCSSC[C@@H](C(N3CCC[C@H]3C(N[C@H](C(NCC(N)=O)=O)CCCN)=O)=O)NC([C@@H](NC([C@H]([C@H](O)C)NC([C@H]([C@H](CC)C)NC2=O)=O)=O)CC(N)=O)=O)=O)cc1
• Target: OXTR
• Solubility: DMSO: <10.3 mg/mL

Bioactivity

• In Vivo:
  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.
  Read more...
• In Vitro:
  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 Ca2+ from the extracellular space through voltage gated channels. In addition, Atosiban suppresses oxytocin-mediated release of PGE and PGF from the decidua.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RW-22164, RWJ-22164

Quick Database Links

Gene Symbol

OXTR