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OT receptor

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Target not currently curated in GtoImmuPdb

Target id: 369

Nomenclature: OT receptor

Family: Vasopressin and oxytocin receptors

Contents:

Gene and Protein Information Click here for help
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 389 3p25.3 OXTR oxytocin receptor 52,54-55,64
Mouse 7 388 6 E3 Oxtr oxytocin receptor 56
Rat 7 388 4q41 Oxtr oxytocin receptor 32,78
Previous and Unofficial Names Click here for help
OTR
Database Links Click here for help
Specialist databases
GPCRdb oxyr_human (Hs), oxyr_mouse (Mm), oxyr_rat (Rn)
Other databases
Alphafold P30559 (Hs), P97926 (Mm), P70536 (Rn)
ChEMBL Target CHEMBL2049 (Hs), CHEMBL3243907 (Mm), CHEMBL3996 (Rn)
DrugBank Target P30559 (Hs)
Ensembl Gene ENSG00000180914 (Hs), ENSMUSG00000049112 (Mm), ENSRNOG00000005806 (Rn)
Entrez Gene 5021 (Hs), 18430 (Mm), 25342 (Rn)
Human Protein Atlas ENSG00000180914 (Hs)
KEGG Gene hsa:5021 (Hs), mmu:18430 (Mm), rno:25342 (Rn)
OMIM 167055 (Hs)
Pharos P30559 (Hs)
RefSeq Nucleotide NM_000916 (Hs), NM_001081147 (Mm), NM_012871 (Rn)
RefSeq Protein NP_000907 (Hs), NP_001074616 (Mm), NP_037003 (Rn)
UniProtKB P30559 (Hs), P97926 (Mm), P70536 (Rn)
Wikipedia OXTR (Hs)
Natural/Endogenous Ligands Click here for help
oxytocin {Sp: Human, Mouse, Rat}
vasopressin {Sp: Human, Mouse, Rat}
Comments: Oxytocin is the principal endogenous ligand
Potency order of endogenous ligands (Human)
oxytocin (OXT, P01178) > vasopressin (AVP, P01185)  [3,23-25,44,50,54]

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Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[3H]AVP (human, mouse, rat) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Partial agonist 8.8 – 8.9 pKd 15,23
⤷ pKd 8.8 – 8.9 [15,23]
[3H]OT (human, mouse, rat) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 8.2 – 9.5 pKd 23,41,50,54
⤷ pKd 8.2 – 9.5 (Kd 6.31x10-9 – 3.16x10-10 M) [23,41,50,54]
arginine vasotocin Peptide Click here for species-specific activity table Hs Full agonist 9.4 pKi 23-24
⤷ pKi 9.4 [23-24]
oxytocin {Sp: Human, Mouse, Rat} Peptide Approved drug Primary target of this compound Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 8.2 – 9.6 pKi 3,23-25,44,50
⤷ pKi 8.2 – 9.6 [3,23-25,44,50]
[Phe3]OT Peptide Click here for species-specific activity table Hs Full agonist 8.8 pKi 23-24
⤷ pKi 8.8 [23-24]
oxytocin {Sp: Human, Mouse, Rat} Peptide Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 8.7 pKi 25
⤷ pKi 8.7 [25]
vasopressin {Sp: Human, Mouse, Rat} Peptide Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Hs Partial agonist 7.3 – 9.3 pKi 3,15,22-24,30,44,50
⤷ pKi 7.3 – 9.3 [3,15,22-24,30,44,50]
dAVP Peptide Click here for species-specific activity table Hs Full agonist 8.3 pKi 22
⤷ pKi 8.3 [22]
[Thr4,Gly7]OT Peptide Click here for species-specific activity table Hs Full agonist 8.2 – 8.4 pKi 18,24,33,50
⤷ pKi 8.2 – 8.4 [18,24,33,50]
d[Cha4]AVP Peptide Click here for species-specific activity table Hs Full agonist 7.1 – 7.7 pKi 30,44
⤷ pKi 7.1 – 7.7 [30,44]
d[Leu4]LVP Peptide Click here for species-specific activity table Rn Full agonist 7.2 pKi 71
⤷ pKi 7.2 [71]
desmopressin Peptide Approved drug Click here for species-specific activity table Hs Full agonist 6.7 – 7.6 pKi 23,50
⤷ pKi 6.7 – 7.6 [23,50]
d[Leu4,Dap8]VP Peptide Click here for species-specific activity table Rn Full agonist 6.9 pKi 71
⤷ pKi 6.9 [71]
d[Leu4]AVP Peptide Click here for species-specific activity table Hs Full agonist 6.7 pKi 22
⤷ pKi 6.7 [22]
LIT-001 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Agonist 6.7 pKi 40
⤷ pKi 6.7 (Ki 2.26x10-7 M) [40]
Description: Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged OT receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
d[Cha4,Dab8]VP Peptide Click here for species-specific activity table Rn Full agonist 6.4 pKi 71
⤷ pKi 6.4 [71]
d[Cha4]LVP Peptide Click here for species-specific activity table Rn Full agonist 6.2 pKi 71
⤷ pKi 6.2 [71]
carbetocin Peptide Approved drug Hs Agonist 8.0 pEC50 40
⤷ pEC50 8.0 (EC50 1x10-8 M) [40]
Description: Agonist activity at hOT receptor receptor expressed in HEK293FT cells by beta-arrestin recruitment assay.
carbetocin Peptide Approved drug Mm Agonist 7.2 pEC50 40
⤷ pEC50 7.2 (EC50 6.2x10-8 M) [40]
Description: Agonist activity at MmOT receptor expressed in HEK293FT cells assessed as stimulation of calcium release by Aequorin based assay.
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[35S]non-peptide OT antagonist Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 10.4 pKd 57
⤷ pKd 10.4 (Kd 4.2x10-11 M) [57]
d(CH2)5[Tyr(Me)2,Thr4,Tyr(3125I)-NH29]OVT Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.7 – 10.0 pKd 15,23-24
⤷ pKd 9.7 – 10.0 [15,23-24]
d(CH2)5[Tyr(Me)2,Thr4,Phe(3125I,4N3)-NH29]OVT Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Antagonist 9.6 pKd 15
⤷ pKd 9.6 [15]
d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT Peptide Click here for species-specific activity table Hs Antagonist 9.2 – 10.0 pKi 44,62
⤷ pKi 9.2 – 10.0 [44,62]
L-366,875 Peptide Hs Antagonist 9.5 pKi 50
⤷ pKi 9.5 [50]
L023103 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.2 pKi 74
⤷ pKi 9.2 [74]
L023103 Small molecule or natural product Rn Antagonist 9.2 pKi 74
⤷ pKi 9.2 [74]
retosiban Small molecule or natural product Primary target of this compound Ligand has a PDB structure Hs Antagonist 9.0 – 9.2 pKi 58,63
⤷ pKi 9.0 – 9.2 (Ki 1x10-9 – 6.5x10-10 M) [58,63]
d(CH2)5[Tyr(Me)2,Thr4,Phe(3I,4N3)-NH29]OVT Peptide Click here for species-specific activity table Hs Antagonist 9.0 pKi 15
⤷ pKi 9.0 [15]
SSR126768A Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.8 – 9.1 pKi 80
⤷ pKi 8.8 – 9.1 (Ki 1.5x10-9 – 9x10-10 M) [80]
compound 37 [PMID: 16250654] Small molecule or natural product Hs Antagonist 8.9 pKi 13
⤷ pKi 8.9 [13]
L-371,257 Small molecule or natural product Hs Antagonist 8.8 pKi 44
⤷ pKi 8.8 [44]
L-366,948 Peptide Hs Antagonist 8.6 pKi 50
⤷ pKi 8.6 [50]
L-365,209 Peptide Hs Antagonist 8.5 pKi 50
⤷ pKi 8.5 [50]
L-368,930 Small molecule or natural product Hs Antagonist 8.5 pKi 50
⤷ pKi 8.5 [50]
L-369,020 Small molecule or natural product Hs Antagonist 8.5 pKi 50
⤷ pKi 8.5 [50]
L-366,682 Peptide Hs Antagonist 8.4 pKi 50
⤷ pKi 8.4 [50]
L-368,228 Small molecule or natural product Hs Antagonist 8.4 pKi 50
⤷ pKi 8.4 [50]
L-372662 Small molecule or natural product Hs Antagonist 8.4 pKi 11
⤷ pKi 8.4 [11]
d(CH2)5[Tyr(Me)2]AVP Peptide Click here for species-specific activity table Hs Antagonist 8.3 pKi 50
⤷ pKi 8.3 [50]
L-368,899 Small molecule or natural product Hs Antagonist 8.1 pKi 50
⤷ pKi 8.1 [50]
L-367,938 Small molecule or natural product Hs Antagonist 7.9 pKi 50
⤷ pKi 7.9 [50]
nelivaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 – 8.8 pKi 44,81
⤷ pKi 6.8 – 8.8 [44,81]
LS-192629 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 – 7.8 pKi 25
⤷ pKi 7.6 – 7.8 [25]
L-367,773 Small molecule or natural product Hs Antagonist 7.6 pKi 50
⤷ pKi 7.6 [50]
atosiban Peptide Approved drug Rn Antagonist 7.1 pKi 25
⤷ pKi 7.1 [25]
LS-192629 Small molecule or natural product Rn Antagonist 6.9 pKi 25
⤷ pKi 6.9 [25]
OPC-21268 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 50
⤷ pKi 6.8 [50]
atosiban Peptide Approved drug Click here for species-specific activity table Hs Antagonist 6.0 – 7.6 pKi 3,25,50,62,80
⤷ pKi 6.0 – 7.6 [3,25,50,62,80]
relcovaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 – 7.0 pKi 3,44
⤷ pKi 6.5 – 7.0 [3,44]
L-366,509 Small molecule or natural product Hs Antagonist 6.6 pKi 50
⤷ pKi 6.6 [50]
balovaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.2 pKi 79
⤷ pKi 5.2 (Ki 7.002x10-6 M) [79]
Ro5028442 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.0 pKi 76
⤷ pKi 5.0 (Ki 9.891x10-6 M) [76]
[Mpa1,D-Tyr(Et)2,D-Tic7,D-Tic9]OT Peptide Hs Antagonist 7.6 pIC50 39
⤷ pIC50 7.6 [39]
[Mpa1,D-Tyr(Et)2,D-Tic7]OT Peptide Hs Antagonist 7.3 pIC50 39
⤷ pIC50 7.3 [39]
[Mpa1,D-Tyr(Et)2,D-Tic7,Aib9]OT Peptide Hs Antagonist 7.1 pIC50 39
⤷ pIC50 7.1 [39]
View species-specific antagonist tables
Immuno Process Associations
Immuno Process:  Cytokine production & signalling
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  83,85
Secondary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gi/Go family Adenylyl cyclase inhibition
References:  85-86
Tissue Distribution Click here for help
Brain and spinal cord: brainstem; dorsal horn of upper spinal cord
Species:  Human
Technique:  Radioligand binding (autoradiography)
References:  61
Vascular endothelial cells.
Species:  Human
Technique:  RT-PCR.
References:  89
Corpus cavernosum
Species:  Human
Technique:  RT-PCR, Northern blotting, immunohistochemistry, Western blotting and radioligand binding.
References:  92
Ovary: cumulus cells.
Species:  Human
Technique:  RT-PCR.
References:  42
Osteoclasts.
Species:  Human
Technique:  Immunofluorescence and Western blotting.
References:  27
Prostate.
Species:  Human
Technique:  In situ hybridisation and immunohistochemistry.
References:  20
Mammary gland.
Species:  Human
Technique:  Immunohistochemistry.
References:  53
Penis.
Species:  Human
Technique:  RT-PCR.
References:  93
Breast tissue.
Species:  Human
Technique:  Immunocytochemistry and RT-PCR.
References:  19
Fetal heart > adult heart.
Species:  Human
Technique:  RT-PCR.
References:  49
Epididymis.
Species:  Human
Technique:  RT-PCR and immunocytochemistry.
References:  38
Osteoblasts.
Species:  Human
Technique:  RT-PCR.
References:  28
Thymic epithelial cells.
Species:  Mouse
Technique:  in situ hybridisation.
References:  46
Uterus.
Species:  Mouse
Technique:  Immunohistochemistry.
References:  12
Brain: ventromedial nucleus of the hypothalamus, central amygdaloid nucleus, the islands of Calleja, olfactory nucleus, lateral septum, dorsal motor nucleus of the vagus nerve, taenia tecta, dorsolateral caudate putamen, ventral pallidum, accumbens, bed nucleus of the stria terminalis, thalamic paraventricular nucleus, lateral, basolateral, and medial amygdala, amygdaloid-hippocampal area.
Species:  Rat
Technique:  Radioligand binding (autoradiography)
References:  34,90
Pituitary
Species:  Rat
Technique:  Northern blotting, RT-PCR and in situ hybridisation
References:  17
CNS: ventromedial hypothalamus.
Species:  Rat
Technique:  in situ hybridisation.
References:  9
Uterus.
Species:  Rat
Technique:  RT-PCR.
References:  26,59,78
Penis.
Species:  Rat
Technique:  RT-PCR, immunohistochemistry, Western blotting and radioligand binding.
References:  97
Thymus
Species:  Rat
Technique:  Radioligand binding
References:  35
Heart.
Species:  Rat
Technique:  in situ hybridisation.
References:  45
Pituitary
Species:  Rat
Technique:  Radioligand binding
References:  6
Mammary gland.
Species:  Rat
Technique:  Radioligand binding.
References:  72,84
Kidney.
Species:  Rat
Technique:  in situ hybridisation.
References:  70
Brain, pituitary, mammary glands, uterus.
Brain: ventromedial hypothalamus, bed nucleus of the stria terminalis, ventral pallidum, paraventricular nucleus, dorsal part of the supraoptic nucleus.
Pituitary: anterior and posterior lobes.
Species:  Rat
Technique:  immunocytochemistry.
References:  1
Testis.
Species:  Rat
Technique:  Radioligand binding.
References:  10
Mammary gland.
Species:  Rat
Technique:  in situ hybridisation.
References:  16
Brain: ventromedial nucleus of the hypothalamus, anterior olfactory nucleus, intermediate bed nucleus of the stria terminalis, frontal cortex, piriform cortex, supraoptic nucleus, arcuate nucleus, suprachiasmatic nucleus, ventral subiculum, cortical amygdala, subfornical organ, mammillary complex > ateral septal nucleus, medial preoptic area, ventral portions of the bed nucleus of the stria terminalis, paraventricular nucleus of the hypothalamus, dorsal caudoputamen, entorhinal cortex, hippocampus, paraventricular nucleus of the thalamus, dorsal raphe, pontine nuclei, substantia nigra pars compacta, ventral tegmental area.
Species:  Rat
Technique:  in situ hybridisation.
References:  69,91
Cardiomyocytes.
Species:  Rat
Technique:  Immunocytochemistry.
References:  49
Expression Datasets Click here for help

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Log average relative transcript abundance in mouse tissues measured by qPCR from Regard, J.B., Sato, I.T., and Coughlin, S.R. (2008). Anatomical profiling of G protein-coupled receptor expression. Cell, 135(3): 561-71. [PMID:18984166] [Raw data: website]

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Functional Assays Click here for help
Measurement of inositol phosphate accumulation in CHO cells transfected with the rat OT receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Stimulation of IP accumulation.
References:  51
Measurement of calcium levels in CHO cells transfected with the rat OT receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Stimulation of calcium mobilisation.
References:  51,83
Measurement of arachidonic acid and PGE2 levels in CHO cells transfected with the rat OT receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Stimulation of arachidonic acid release followed by PGE2 synthesis.
References:  51
Measurement of ERK2 phosphorylation in CHO cells transfected with the rat OT receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Stimulation of ERK2 phosphorylation.
References:  85
Physiological Functions Click here for help
Inhibition of food and water intake.
Species:  Rat
Tissue:  In vivo.
References:  7,67
Milk ejection.
Species:  Mouse
Tissue:  In vivo.
References:  66,96
Stimulation of parturition.
Species:  Rat
Tissue:  In vivo.
References:  5,21,75
Uterine contractions.
Species:  Rat
Tissue:  In vivo.
References:  2,63
Muscle contractions.
Species:  Human
Tissue:  Myometrium strips.
References:  73,94
Muscle contractions.
Species:  Rat
Tissue:  Myometrium strips.
References:  8,36
Noradrenaline release.
Species:  Rat
Tissue:  In vivo (supraoptic nucleus).
References:  68
Modulation of exercise-induced tachycardia.
Species:  Rat
Tissue:  In vivo (heart).
References:  14
Cardiomyogenesis.
Species:  Rat
Tissue:  Heart.
References:  49
Facilitation of sperm transport during ejaculation.
Species:  Human
Tissue:  In vivo (epididymis).
References:  38
Stimulation of renin secretion.
Species:  Rat
Tissue:  In vivo (kidney).
References:  47,60,82
Stimulation of urinary Na+ excretion in response to continual (not pulsatile) administration of oxytocin.
Species:  Rat
Tissue:  In vivo (kidney).
References:  82
Regulation of stress-induced antinociception.
Species:  Mouse
Tissue:  Dorsal horn neurones in spinal slices.
References:  77
Attenuation of stress-induced hypothalamic-pituitary-adrenal axis activity.
Species:  Rat
Tissue:  In vivo.
References:  65,95
Development of social memory.
Species:  Mouse
Tissue:  In vivo.
References:  29,37
Physiological Consequences of Altering Gene Expression Click here for help
Female OT receptor knockout mice exhibit defects in lactation and maternal nuturing; male OT receptor knockout mice have deficits in social discrimination and elevated aggressive behaviour.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  87
Phenotypes, Alleles and Disease Models Click here for help Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
Oxtrtm1Wsy Oxtrtm1Wsy/Oxtrtm1Wsy
involves: 129S1/Sv * 129X1/SvJ		 MGI:109147  MP:0002152 abnormal brain morphology PMID: 18356275 
Oxtrtm1.1Knis Oxtrtm1.1Knis/Oxtrtm1.1Knis
involves: 129P2/OlaHsd * C57BL/6J		 MGI:109147  MP:0001386 abnormal maternal nurturing PMID: 16249339 
Oxtrtm1.2Wsy Oxtrtm1.2Wsy/Oxtrtm1.2Wsy
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * CBA * SJL		 MGI:109147  MP:0003838 abnormal milk ejection PMID: 18356275 
Oxtrtm1.1Knis Oxtrtm1.1Knis/Oxtrtm1.1Knis
involves: 129P2/OlaHsd * C57BL/6J		 MGI:109147  MP:0001384 abnormal pup retrieval PMID: 16249339 
Oxtrtm1.1Knis Oxtrtm1.1Knis/Oxtrtm1.1Knis
involves: 129P2/OlaHsd * C57BL/6J		 MGI:109147  MP:0001360 abnormal social investigation PMID: 16249339 
Oxtrtm1.1Wsy|Tg(Camk2a-cre)1Szi Oxtrtm1.1Wsy/Oxtrtm1.1Wsy,Tg(Camk2a-cre)1Szi/0
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * CBA * SJL		 MGI:109147  MGI:2177766  MP:0001360 abnormal social investigation PMID: 18356275 
Oxtrtm1.2Wsy Oxtrtm1.2Wsy/Oxtrtm1.2Wsy
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * CBA * SJL		 MGI:109147  MP:0001360 abnormal social investigation PMID: 18356275 
Oxtrtm1.1Knis Oxtrtm1.1Knis/Oxtrtm1.1Knis
involves: 129P2/OlaHsd * C57BL/6J		 MGI:109147  MP:0001529 abnormal vocalization PMID: 16249339 
Oxtrtm1.1Knis Oxtrtm1.1Knis/Oxtrtm1.1Knis
involves: 129P2/OlaHsd * C57BL/6J		 MGI:109147  MP:0009326 absent maternal crouching PMID: 16249339 
Oxtrtm1.1Wsy|Tg(Camk2a-cre)1Szi Oxtrtm1.1Wsy/Oxtrtm1.1Wsy,Tg(Camk2a-cre)1Szi/0
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * CBA * SJL		 MGI:109147  MGI:2177766  MP:0001262 decreased body weight PMID: 18356275 
Oxtr+|Oxtrtm1.2Wsy Oxtrtm1.2Wsy/Oxtr+
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * CBA * SJL		 MGI:109147  MP:0001935 decreased litter size PMID: 18356275 
Oxtrtm1.1Knis Oxtrtm1.1Knis/Oxtrtm1.1Knis
involves: 129P2/OlaHsd * C57BL/6J		 MGI:109147  MP:0001399 hyperactivity PMID: 16249339 
Oxtrtm1.1Knis Oxtrtm1.1Knis/Oxtrtm1.1Knis
involves: 129P2/OlaHsd * C57BL/6J		 MGI:109147  MP:0001353 increased aggression towards mice PMID: 16249339 
Oxtrtm1.1Knis Oxtrtm1.1Knis/Oxtrtm1.1Knis
involves: 129P2/OlaHsd * C57BL/6J		 MGI:109147  MP:0010249 lactation failure PMID: 16249339 
Oxtrtm1.1Wsy Oxtrtm1.1Wsy/Oxtrtm1.1Wsy
involves: 129S1/Sv * 129X1/SvJ * C57BL/6 * SJL		 MGI:109147  MP:0002169 no abnormal phenotype detected PMID: 18356275 
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphism
Species:  Human
Description:  SNPs in the OT receptor gene may be linked to autism.
SNP accession:  rs2254298
References:  48
General Comments
The number of OT receptors in the uterus increases near to parturition [26].

The neurohypophysial hormone oxytocin (OT) was the first peptide hormone to have its structure determined and the first to be chemically synthesised in biologically active form [31]. Circulating OT is associated chiefly with the contraction of uterine smooth muscle at term and of myoepithelial cells that surround the alveoli of the mammary gland during lactation through its action on OT receptors. Today, it is recognised that OT exerts a wide spectrum of central and peripheral effects. These actions of OT range from the modulation of neuroendocrine reflexes to the establishment of complex social and bonding behaviours related to the reproduction and care of the offspring [43]. OT receptors form homodimers in vitro and may heterodimerise with vasopressin V1A and V2 receptors [88].

A peptide antagonist, [1-deamino,D-Tyr(Et)2,Thr4,Orn8]vasotocin (atosiban), shown to inhibit uterine contractions in women, threatened and established pre-term labour [4], has been approved for clinical use in Europe.

References

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1. Adan RA, Van Leeuwen FW, Sonnemans MA, Brouns M, Hoffman G, Verbalis JG, Burbach JP. (1995) Rat oxytocin receptor in brain, pituitary, mammary gland, and uterus: partial sequence and immunocytochemical localization. Endocrinology, 136 (9): 4022-8. [PMID:7649111]

2. Ahn TG, Han SJ, Cho YS, An TH, Pak SC, Flouret G. (2004) In vivo activity of the potent oxytocin antagonist on uterine activity in the rat. In Vivo, 18 (6): 763-6. [PMID:15646817]

3. Akerlund M, Bossmar T, Brouard R, Kostrzewska A, Laudanski T, Lemancewicz A, Serradeil-Le Gal C, Steinwall M. (1999) Receptor binding of oxytocin and vasopressin antagonists and inhibitory effects on isolated myometrium from preterm and term pregnant women. Br J Obstet Gynaecol, 106 (10): 1047-53. [PMID:10519430]

4. Akerlund M, Carlsson AM, Melin P, Trojnar J. (1985) The effect on the human uterus of two newly developed competitive inhibitors of oxytocin and vasopressin. Acta Obstet Gynecol Scand, 64 (6): 499-504. [PMID:4061066]

5. Alexandrova M, Soloff MS. (1980) Oxytocin receptors and parturition. I. Control of oxytocin receptor concentration in the rat myometrium at term. Endocrinology, 106 (3): 730-5. [PMID:6243547]

6. Antoni FA. (1986) Oxytocin receptors in rat adenohypophysis: evidence from radioligand binding studies. Endocrinology, 119 (5): 2393-5. [PMID:3021442]

7. Arletti R, Benelli A, Bertolini A. (1990) Oxytocin inhibits food and fluid intake in rats. Physiol Behav, 48 (6): 825-30. [PMID:2087513]

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