oxytocin receptor

OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist.

OT-R antagonist 2 is a nonpeptide low molecular weight antagonist of OT-R .

d[Cha4]-AVP acetate is a potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). Stimulates ACTH and corticosterone secretion and exhibits negligible vasopr

Oxytocin C-terminal tripeptide Acetate is the C-terminal tripeptide of Oxytocin.Oxytocin is a mammalian neuropituitary hormone, a ligand for the 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 is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth.

PF-06655075 (TFA) is the trifluoroacetic acid (TFA) salt of PF-06655075, a novel, non-brain-penetrant oxytocin receptor agonist that exhibits 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].

Selective vasopressin V1B receptor agonist (Ki values are 0.16, 64, 100 and 3800 nM for V1B, oxytocin, V2 and V1A receptors respectively). Displays weak antidiuretic, vasopressor and in vitro oxytocic activities.

Merotocin is a potent and highly selective peptidic agonist of the oxytocin receptor.

Erlosiban, also known as OBE001, is a novel, orally active nonpeptide oxytocin receptor antagonist under development for the treatment of preterm labor and improvement in embryo implantation and pregnancy rate in assisted reproductive technology (ART).

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

oxytocin receptor partial agonist

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

d[Cha4]-AVP TFA is a potent and selective agonist for the vasopressin (AVP) V1b receptor, displaying a high affinity with a K i of 1.2 nM. It exhibits greater selectivity for the V1b receptor over the V1a receptor, V2 receptor, and oxytocin receptors, demonstrating its specificity in targeting the human V1b receptor [1] [2].

(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].

Potent and selective human vasopressin V1B receptor agonist (Ki values are 1.2, 151, 240 and 750 nM for V1B, V1A, Oxytocin and V2 receptors respectively). Stimulates ACTH and corticosterone secretion and exhibits negligible vasopressor activity in vivo.

L 366948 is an antagonist of the oxytocin receptor.

Epelsiban Besylate is an oral drug that is a highly selective anamol oxytocin receptor antagonist.

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.

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].

Val9-Oxytocin, an Oxytocin analog where Gly9 is substituted with Val9 [1], functions as a complete antagonist of the vasopressin (V1a) receptor.

Ota-vasotocin is a ligand utilized in quantitative receptor autoradiography for oxytocin receptors.

L-368899 is a non-peptide and orally active antagonist of oxytocin receptor (IC50: 8.9 nM). It displays 40-fold selectivity over vasopressin V1a and V2 receptors (IC50: 370 and 570 nM respectively).

ALS-I-41 is a novel, potent and selective antagonist of oxytocin receptor.

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.

Barusiban is an 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.

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].

LIT-001 free base improves social interaction in a mouse model of autism. LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM).

(Thr4,Gly7)-Oxytocin, an analogue of Oxytocin and a specific OT receptor agonist, not only activates TRPV1 channels to excite subicular neurons but also reduces the activity of potassium (K+) channels. [1] [2].

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

Oxytocin (Oxytocin (Syntocinon)) is a mammalian neurohypophysial hormone, a ligand of oxytocin receptor.

(d(CH2)51,Tyr(Me)2, Orn8)-Oxytocin (OVT) is an antagonist of the oxytocin receptor that finds application in the study of neurological diseases [1].

SHR1653 is a highly potent, selective and brain penetrated antagonist of oxytocin receptor (OTR)(IC50 of 15 nM for hOTR).

oxytocin receptor (OTR) agonist

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.

Selective vasopressin V1A receptor antagonist. Inhibits vasopressin and oxytocin-induced increases in intracellular calcium concentrations in vitro (IC50 values are 5 and 30 nM respectively). Exhibits potent and prolonged antivasopressor activity and indu

Epelsiban is a selective and orally bioavailable oxytocin receptor antagonist (pKi: 9.9 for human oxytocin receptor).