1. Signaling Pathways
  2. GPCR/G Protein
  3. Oxytocin Receptor

Oxytocin Receptor

OXTR

The oxytocin receptor belongs to the G-protein-coupled seven-transmembrane receptor superfamily. Its main physiological role is regulating the contraction of uterine smooth muscle at parturition and the ejection of milk from the lactating breast. The oxytocin receptors are activated in response to binding oxytocin and a similar nonapeptide, vasopressin. Oxytocin receptor triggers Gi or Gq protein-mediated signaling cascades leading to the regulation of a variety of neuroendocrine and cognitive functions.

Oxytocin is a nonapeptide of the neurohypophyseal protein family that binds specifically to the oxytocin receptor to produce a multitude of central and peripheral physiological responses. In vivo, oxytocin acts as a paracrine and/or autocrine mediator of multiple biological effects. These effects are exerted primarily through interactions with G-protein-coupled oxytocin/vasopressin receptors, which, via Gq and Gi, stimulate phospholipase C-mediated hydrolysis of phosphoinositides.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-P5213
    Vasopressin Dimer (parallel) TFA
    Activator 99.55%
    Vasopressin Dimer (parallel) TFA is a parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR.
    Vasopressin Dimer (parallel) TFA
  • HY-P2168
    Demoxytocin
    98.34%
    Demoxytocin is a heterologous cyclic peptide and an analog of Oxytocin (HY-17571). Demoxytocin affects the permeability of cell membranes and increases calcium ion levels in smooth muscle cells, thereby enhancing the contraction of smooth muscle cells. Demoxytocin also stimulates the contraction of uterine smooth muscle. Demoxytocin possesses the functions of oxytocin. Demoxytocin can be used to study labor stimulation in preterm premature rupture of membranes.
    Demoxytocin
  • HY-105018
    Epelsiban
    Antagonist
    Epelsiban (GSK 557296) is a potent, selective and orally bioavailable oxytocin receptor antagonist, with a pKi of 9.9 for human oxytocin receptor.
    Epelsiban
  • HY-P3866
    [Asu1,6]-Oxytocin
    [Asu1,6]-Oxytocin is an analog of oxytocin. [Asu1,6]-Oxytocin reverses insulin resistance and glucose intolerance prior to reduction of obesity. [Asu1,6]-Oxytocin has the potential for the research of obesity and diabetes.
    [Asu1,6]-Oxytocin
  • HY-15007
    L 366509
    Antagonist
    L 366509 is a spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist. Modifications led to a new series of o-tolylpiperazine (TP) camphorsulfonamides, exhibiting high affinity for OT receptors and selectivity over arginine vasopressin receptors. Notably, compound 7 (L-368,899) showed excellent OT receptor affinity, potency in inhibiting OT-stimulated uterine contractions, good aqueous solubility, and oral bioavailability in multiple species. Compound 7 has entered clinical testing as an oral and intravenous tocolytic agent. Molecular modeling suggests the TP camphorsulfonamide structure mimics the D-AA2-Ile3 dipeptide, crucial in potent OT antagonists.
    L 366509
  • HY-153964A
    PF-06478939 TFA
    Agonist
    PF-06478939 TFA is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC50 values of 0.01 nM and 0.078 nM, respectively.
    PF-06478939 TFA
  • HY-103649
    OT antagonist 3
    Antagonist
    OT antagonist 3 is an oxytocin (OT) antagonist extracted from patent WO2007017752A1.
    OT antagonist 3
  • HY-P2034
    Cargutocin
    Cargutocin, an oxytocin analogue, targets the oxytocin receptor and acts as a uterine contraction agent.
    Cargutocin
  • HY-P3516
    Barusiban
    Antagonist
    Barusiban (FE-200440) is an oxytocin receptor (OT-R) antagonist (Ki=0.8 nM), inhibits OT-induced contraction. Barusiban can be used in preterm labor (PTL), in vitro fertilisation (IVF) and infertility research.
    Barusiban
  • HY-120301
    L-366682
    Inhibitor
    L-366682, a cyclic hexapeptide, possesses antagonism of oxytocin.
    L-366682
  • HY-153964
    PF-06478939
    Agonist
    PF-06478939 is a non-brain-penetrating peptide that is an agonist at oxytocin (OT) receptor and vasopressin receptor with EC50 values of 0.01 nM and 0.078 nM, respectively.
    PF-06478939
  • HY-103652
    OT antagonist 3 analog
    Antagonist
    OT antagonist 3 analog is an analog of OT antagonist 3.
    OT antagonist 3 analog
  • HY-P3220
    [D-Asn5]-Oxytocin
    Activator
    [D-Asn5]-Oxytocin possesses very low specific oxytocic and vasodepressor activities. By cumulative dose-response studies for oxytocic activity, [D-Asn5]-Oxytocin has similar intrinsic activity to oxytocin.
    [D-Asn5]-Oxytocin
  • HY-15008
    L-368,899
    Antagonist
    L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor.
    L-368,899
  • HY-P5017
    (Val3,Pro8)-Oxytocin
    Agonist
    (Val3,Pro8)-Oxytocin is the Gq-dependent pathway agonist. (Val3,Pro8)-Oxytocin is also a weaker agonist for the β-arrestin engagement and endocytosis toward the oxytocin receptor (OXTR).
    (Val3,Pro8)-Oxytocin
  • HY-P3216
    Oxytocin free acid
    Agonist
    Oxytocin free acid (9-Deamidooxytocin) is an analog of oxytocin in which the glycinamide residue at position 9 in oxytocin has been replaced by a glycine residue. Oxytocin is a pleiotropic, peptide hormone with broad implications for general health, adaptation, development, reproduction, and social behavior.
    Oxytocin free acid
  • HY-P5214
    Vasopressin Dimer (anti-parallel) TFA
    Activator
    Vasopressin Dimer (anti-parallel) TFA is an anti-parallel dimer of Vasopressin (HY-B1811). Vasopressin Dimer (anti-parallel) TFA can activate four G protein-coupled receptors, V1aR, V1bR, V2R, and OTR.
    Vasopressin Dimer (anti-parallel) TFA
  • HY-P4703
    Hydrin 1′
    Hydrin 1′ is found in the neurohypophysis of Xenopus. Hydrin 1′ possesses a considerable steroid-releasing activity in Xenopus adrenal gland in vitro. Hydrin 1′ targets oxytocin receptor and derives a fluorescent probe of the oxytocin receptor.
    Hydrin 1′
  • HY-124391
    L 156373
    Antagonist
    L 156373 is a potent oxytocin receptor antagonist with Ki value of 150 nM.
    L 156373
  • HY-153963A
    PF-06655075 TFA
    Agonist
    PF-06655075 (TFA) is the TFA form of PF-06655075 (HY-153963). PF-06655075 is a novel andnon–brain-penetrant oxytocin receptor agonist with increased selectivity for the oxytocin receptor and significantly increased pharmacokinetic stability. PF-06655075 can be used as a tool compound to further explore the role of peripheral oxytocin in behavioral response.
    PF-06655075 TFA
Cat. No. Product Name / Synonyms Application Reactivity