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-17571A
    Oxytocin acetate
    		Agonist 99.69%
    Oxytocin (α-Hypophamine) acetate is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin acetate can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma.
    Oxytocin acetate
  • HY-108677
    L-368,899 hydrochloride
    		Antagonist 98.78%
    L-368,899 hydrochloride is a potent, selective, orally bioavailable, non-peptide oxytocin receptor antagonist, with IC50s of 8.9 nM and 26 nM for rat uterus and human uterus oxytocin receptor, respectively. L-368,899 hydrochloride used as a tocolytic agent.
    L-368,899 hydrochloride
  • HY-17571
    Oxytocin
    		Agonist 99.79%
    Oxytocin (α-Hypophamine; Oxytocic hormone) is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma.
    Oxytocin
  • HY-17572A
    Atosiban acetate
    		Antagonist 99.88%
    Atosiban acetate (RW22164 acetate;RWJ22164 acetate) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.
    Atosiban acetate
  • HY-124733A
    LIT-001
    		Agonist 98.14%
    LIT-001 is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 improves social interaction in a mouse model of autism.
    LIT-001
  • 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-124391
    L 156373
    		Antagonist
    L 156373 is an oxytocin receptor antagonist with Ki value of 150 nM.
    L 156373
  • 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-17573
    Carbetocin
    		Agonist 99.97%
    Carbetocin, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin has the potential for postpartum hemorrhage research. Carbetocin can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
    Carbetocin
  • HY-P3467
    (Thr4,Gly7)-Oxytocin
    		Agonist 99.82%
    (Thr4,Gly7)-Oxytocin, an Oxytocin analogue, is a specific OT receptor agonist. (Thr4,Gly7)-Oxytocin also excites subicular neurons via activation of TRPV1 channels, and depression of K+ channels. .
    (Thr4,Gly7)-Oxytocin
  • HY-17572
    Atosiban
    		Antagonist 99.55%
    Atosiban (RW22164; RWJ22164) is a nonapeptide competitive vasopressin/oxytocin receptor antagonist, and is a desamino-oxytocin analogue. Atosiban is the main tocolytic agent and has the potential for spontaneous preterm labor research.
    Atosiban
  • HY-15010
    L-371,257
    		Antagonist 99.90%
    L-371,257 is an orally bioavailable, non-blood-brain barrier penetrant, selective and competitive antagonist of oxytocin receptor (pA2=8.4) with high affinity at both the oxytocin receptor (Ki=19 nM) and vasopressin V1a receptor (Ki=3.7 nM).
    L-371,257
  • HY-15023
    Cligosiban
    		Antagonist 99.88%
    Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents[1][2].
    Cligosiban
  • HY-14778
    Retosiban
    		Antagonist 98.97%
    Retosiban (GSK221149A) is a potent and selective oxytocin antagonist with a Ki of 0.65 nM.
    Retosiban
  • HY-P3217
    [Asp5]-Oxytocin
    		Agonist 99.19%
    [Asp5]-Oxytocin is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity. [Asp5]-Oxytocin causes uterine contractions in vitro, enhanced by Mg2+. [Asp5]-Oxytocin has the ability of rat uteroconstrictor, avian vasodilator, and rat antidiuretic.
    [Asp5]-Oxytocin
  • HY-17573A
    Carbetocin acetate
    		Agonist 99.81%
    Carbetocin acetate, an oxytocin (OT) analogue, is an oxytocin receptor agonist with a Ki of 7.1 nM. Carbetocin acetate has high affinity to chimeric N-terminus (E1) of the oxytocin receptor (Ki=1.17 μM). Carbetocin acetate has the potential for postpartum hemorrhage research. Carbetocin acetate can crosse the blood-brain barrier and produces antidepressant-like activity via activation of oxytocin receptors in the CNS.
    Carbetocin acetate
  • HY-128351
    SHR1653
    		Antagonist 99.69%
    SHR1653 is a highly potent, selective and brain penetrated oxytocin receptor (OTR) antagonist, with an IC50 of 15 nM for hOTR.
    SHR1653
  • HY-15015A
    OT-R antagonist 2
    		Antagonist 99.86%
    OT-R antagonist 2 is a nonpeptide low molecular weight OT-R antagonist.
    OT-R antagonist 2
  • HY-153963
    PF-06655075
    		Agonist 99.24%
    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-P3217A
    [Asp5]-Oxytocin acetate
    		Agonist 99.13%
    [Asp5]-Oxytocin acetate is the first 5-position neurohypophyseal hormone analogue possessing significant biological activity. [Asp5]-Oxytocin acetate causes uterine contractions in vitro, enhanced by Mg2+. [Asp5]-Oxytocin acetate has the ability of rat uteroconstrictor, avian vasodilator, and rat antidiuretic.
    [Asp5]-Oxytocin acetate
Cat. No. Product Name / Synonyms Application Reactivity