Atosiban (acetate)

Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research^[1]. 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^[1]. 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^[1].
Atosiban blocks the activation of oxytocin-receptor-expressing neurons in the parabrachial nucleus of mice^[2].