Oxytocin Receptor

Oxytocin (Syntocinon) is a mammalian neuropituitary hormone, a pleiotropic hypothalamic peptide and ligand for the oxytocin receptor, which contributes to labor, lactation, and pro-social behavior. Oxytocin has the ability to stimulate mammary secretion of breast milk, promote contraction of uterine smooth muscle during labor, and facilitate mothering.

L-371,257 is a competitive antagonist of oxytocin receptor with pA2 of 8.4 and Ki of 19 nM. L-371,257 shows a Ki of 3.7 nM for vasopressin receptor 1a.

SSR126768A is a novel and selective, orally active and potent oxytocin (OT) receptor antagonist with inhibitory effects on uterine contractions for the prevention of preterm labor.

Atosiban acetate (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban acetate (RW22164) inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. 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 acetate (RW22164) suppresses oxytocin-mediated release of PGE and PGF from the decidua. In human pre-term labor, atosiban, at the recommended dosage, antagonizes 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.

Carbetocin acetate is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

Oxytocin acetate (α-Hypophamine acetate) is a mammalian neurohypophysial hormone, a ligand of oxytocin receptor.

LIT-001 improves social interaction in a mouse model of autism.It is the first nonpeptide oxytocin receptor agonist with EC50 of 55 nM and Ki of 226 nM.

Carbetocin is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

Atosiban (RW22164) is an inhibitor of the hormones oxytocin and vasopressin. It is used as an intravenous medication as a labour repressant (tocolytic) to halt premature labor. Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane. 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. In human pre-term labor, atosiban, at the recommended dosage, antagonizes 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.

Pro8-Oxytocin TFA, a modified oxytocin (OXT) ligand, exhibits greater potency and efficacy than the standard mammalian OXT ligand, Leu8-Oxytocin, at primate OXTR and elicits more pronounced behavioral effects. Compared to vasopressin (AVP), Pro8-Oxytocin TFA has a lower efficacious response at human AVPR1a, yet shows a higher efficacy at the marmoset AVPR1a [1].

Pro8-Oxytocin, a modified oxytocin (OXT) ligand, elicits more potent and efficacious responses at primate OXTR and induces stronger behavioral effects compared to the standard mammalian OXT ligand (Leu8-Oxytocin). It demonstrates lower efficacy than Vasopressin (AVP) at human AVPR1a, yet shows a higher efficacious response at marmoset AVPR1a [1].

PF-06478939 TFA is a peptide that acts as a non-brain-penetrating agonist at the oxytocin (OT) and vasopressin receptors, exhibiting EC50 values of 0.01 nM and 0.078 nM, respectively [1].

PF-06655075 (TFA) is the trifluoroacetic acid (TFA) salt of PF-06655075, a novel non-brain-penetrant oxytocin receptor agonist with enhanced selectivity for the oxytocin receptor and improved pharmacokinetic stability. It serves as a valuable tool compound for investigating the influence of peripheral oxytocin on behavioral responses [1].

(d(CH2)51,Tyr(Me)2, Orn8)-Oxytocin (OVT) is an oxytocin receptor antagonist used in neurological disease research [1].

PF-06655075 is a novel, non-brain-penetrant oxytocin receptor agonist that demonstrates enhanced selectivity for the oxytocin receptor and substantially improved pharmacokinetic stability. This compound serves as a tool to further investigate the function of peripheral oxytocin in behavioral responses [1].

PF-06478939 is a peptide that functions as an agonist at the oxytocin (OT) receptor and vasopressin receptor without crossing the blood-brain barrier. It exhibits EC50 values of 0.01 nM at the OT receptor and 0.078 nM at the vasopressin receptor [1].

(Val3,Pro8)-Oxytocin functions primarily as a Gq-dependent pathway agonist and exhibits secondary activity as a reduced efficacy agonist for β-arrestin recruitment and receptor-mediated endocytosis at the oxytocin receptor (OXTR) [1].