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-368,899 hydrochloride is an orally available and selective nonpeptide oxytocin receptor (OXTR) antagonist for the prevention of preterm labor.L-368,899 hydrochloride prevents oxytocin-induced anti-anomalous pain and anti-nausea, and may be useful for the study of depression.

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.

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.

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

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.

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

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.

PF3274167 (Cligosiban) is a potent and selective, high-affinity nonpeptide oxytocin receptor antagonist.

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.

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

L 364918 is an oxytocin antagonist.

L-366,509 is an antagonist of oxytocin.

L-372662 is bioactive chemical.

oxytocin receptor partial agonist

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].

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].

(D(CH2)51,Tyr(Me)2,Thr4,Orn8,des-Gly-NH29)-Vasotocin, serving as an oxytocin receptor antagonist, effectively nullifies the augmentation of inhibitory postsynaptic currents in CA1 pyramidal neurons by oxytocin [1].

Vasopressin Dimer (anti-parallel) TFA, an anti-parallel dimer form of vasopressin, has the capability to activate four G protein-coupled receptors: V1aR, V1bR, V2R, and OTR [1].

Lysipressin ([Lys8]-Vasopressin), Induces contraction of the rabbit urinary bladder smooth muscle, activate adenylate-cyclase. Lysipressin is Antidiuretic hormone that have been found in pigs and some marsupial families.

Oxytocin parallel dimer is a homo peptide dimer connected by a disulfide bridge.

5β-Dihydroprogesterone (5β-DHP) is a progesterone receptor agonist and metabolite of progesterone .1,2It is formed from progesterone by 5β-reductase.25β-DHP inhibits spontaneous contractions in isolated rat uterus when used at a concentration of 10 μg/ml, an effect that can be blocked by the progesterone receptor antagonist RU486 but not the GABAAreceptor antagonist picrotoxin .1It is a negative modulator of homooligomeric Ρ1 subunit-containing GABAAreceptors, inhibiting GABA-induced currents inX. laevisoocytes expressing these receptors (IC50= 5.02 μM).3Plasma levels of 5β-DHP decrease at the onset of spontaneous human labor.4

L 365209 is an oxytocin antagonist.

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].