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  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-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-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-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-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-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-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
  • HY-15018A
    SSR126768A free base
    Antagonist
    SSR126768A free base is an orally active antagonist for oxytocin receptor, with Ki of 0.44 nM. SSR126768A free base is a tocolytic agent, that antagonizes the Oxytocin (HY-17571)-induced intracellular Ca2+ increase and prostaglandin release in human uterine smooth muscle cells, inhibits thus the Oxytocin (HY-17571)-induced uterine contraction and delays parturition in pregnant rats in labor.
    SSR126768A free base
  • 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
Cat. No. Product Name / Synonyms Application Reactivity