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

Oxytocin Receptor

OXTR

Oxytocin Receptor

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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-108678
    TC OT 39
    		Agonist
    TC OT 39 is a synthetic oxytocin analog, as well as a selective agonist of oxytocin receptor (OXTR, EC50=180 nM). TC OT 39 is also an Avprla vasopressin receptor antagonist with an Ki value of 330 nM. TC OT 39 exhibits sedative effects in mouse models.
    TC OT 39
  • 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-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-153963
    PF-06655075
    		Agonist
    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
  • HY-P4990A
    Pro8-Oxytocin TFA
    		Activator
    Pro8-Oxytocin TFA is a a modified oxytocin (OXT) ligand. Pro8-Oxytocin produces more potent and efficacious responses at primate OXTR and stronger behavioral effects than the consensus mammalian OXT ligand (Leu8-Oxytocin). Pro8-Oxytocin TFA produce a less efficacious response than Vasopressin (HY-B1811) (AVP) at human AVPR1a and higher efficacious response than AVP at marmoset AVPR1a.
    Pro8-Oxytocin 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-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-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-124733
    LIT-001 free base
    		Agonist
    LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 free base improves social interaction in a mouse model of autism.
    LIT-001 free base
  • 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-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-15522
    WAY-267464
    		Agonist
    WAY-267464 is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder.
    WAY-267464
  • HY-P4990
    Pro8-Oxytocin
    		Activator
    Pro8-Oxytocin is a a modified oxytocin (OXT) ligand. Pro8-Oxytocin produces more potent and efficacious responses at primate OXTR and stronger behavioral effects than the consensus mammalian OXT ligand (Leu8-Oxytocin). Pro8-Oxytocin produce a less efficacious response than Vasopressin (HY-B1811) (AVP) at human AVPR1a and higher efficacious response than AVP at marmoset AVPR1a.
    Pro8-Oxytocin
  • HY-P4895
    (d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin
    		Antagonist
    (d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin (OVT) is an oxytocin receptor antagonist. (d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin can be used for the research of neurological disease.
    (d(CH2)51,Tyr(Me)2,Orn8)-Oxytocin
  • HY-103650
    OT antagonist 1
    		Antagonist
    OT antagonist 1 (Compound 4) is a potent, selective Oxytocin antagonist with a Ki of 50 nM.
    OT antagonist 1
  • HY-108679
    WAY-267464 hydrochloride
    		Agonist
    WAY-267464 hydrochloride is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 hydrochloride can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 hydrochloride can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder.
    WAY-267464 hydrochloride
  • HY-P2014
    (d(CH2)51,Tyr(Me)2,Thr4,Orn8,Tyr-NH29)-Vasotocin
    		Antagonist
    (d(CH2)51,Tyr(Me)2,Thr4,Orn8,Tyr-NH29)-Vasotocin is an oxytocin antagonist and can be used for the research of sexual behavior.
    (d(CH2)51,Tyr(Me)2,Thr4,Orn8,Tyr-NH29)-Vasotocin
  • HY-15011
    L-372662
    		Antagonist 98.70%
    L-372662 is a potent and orally active non-peptide oxytocin antagonist with a Ki value of 4.8. The Kd value of L-372662 for wild-type hOTR and [A318G]OTR is 5.8 nM and 73 nM. L-372662 shows selectivity to OTR:V1aR.
    L-372662
Cat. No. Product Name / Synonyms Application Reactivity