Retosiban (GSK-221149; GSK-221149A) is a novel, potent, orally bioactive, and selective, sub-nanomolar oxytocin receptor antagonist with Ki of 0.65 nM and >1400-fold selectivity over the related vasopressin receptors.

Atosiban acetate, the acetate salt of Atosiban (RW-22164; Tractocile; RWJ22164), is a novel and potent peptide-based oxytocin and vasopressin antagonist with the potential to be used for spontaneous preterm labor.

Carbetocin is a novel and potent obstetric drug acting as an agonist of the oxytocin receptor (Ki of 7.1 nM) with improved in vivo stability over oxytocin. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier […]