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V1A receptor

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Target not currently curated in GtoImmuPdb

Target id: 366

Nomenclature: V1A 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 7 418 12q14.2 AVPR1A arginine vasopressin receptor 1A 79-80
Mouse 7 423 10 D2 Avpr1a arginine vasopressin receptor 1A 37
Rat 7 424 7q22 Avpr1a arginine vasopressin receptor 1A 47
Previous and Unofficial Names Click here for help
V1aR | AVPR1 | antidiuretic hormone receptor 1a | AVPR | AVPR1A
Database Links Click here for help
Specialist databases
GPCRdb v1ar_human (Hs), v1ar_mouse (Mm), v1ar_rat (Rn)
Other databases
Alphafold P37288 (Hs), Q62463 (Mm), P30560 (Rn)
ChEMBL Target CHEMBL1889 (Hs), CHEMBL3414410 (Mm), CHEMBL2868 (Rn)
DrugBank Target P37288 (Hs)
Ensembl Gene ENSG00000166148 (Hs), ENSMUSG00000020123 (Mm), ENSRNOG00000004400 (Rn)
Entrez Gene 552 (Hs), 54140 (Mm), 25107 (Rn)
Human Protein Atlas ENSG00000166148 (Hs)
KEGG Gene hsa:552 (Hs), mmu:54140 (Mm), rno:25107 (Rn)
OMIM 600821 (Hs)
Pharos P37288 (Hs)
RefSeq Nucleotide NM_000706 (Hs), NM_016847 (Mm), NM_053019 (Rn)
RefSeq Protein NP_000697 (Hs), NP_058543 (Mm), NP_444178 (Rn)
UniProtKB P37288 (Hs), Q62463 (Mm), P30560 (Rn)
Wikipedia AVPR1A (Hs)
Natural/Endogenous Ligands Click here for help
oxytocin {Sp: Human, Mouse, Rat}
vasopressin {Sp: Human, Mouse, Rat}
Comments: Vasopressin is the principal endogenous agonist
Potency order of endogenous ligands (Human)
vasopressin (AVP, P01185) > oxytocin (OXT, P01178)  [1,16,20,51,60,72,79]

Download all structure-activity data for this target as a CSV file go icon to follow link

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 Full agonist 8.6 – 10.2 pKd 9,17,71-72,79
⤷ pKd 8.6 – 10.2 (Kd 2.51x10-9 – 6.3x10-11 M) [9,17,71-72,79]
F180 Peptide Hs Full agonist 7.9 – 8.3 pKd 2,20
⤷ pKd 7.9 – 8.3 [2,20]
[3H]OT (human, mouse, rat) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 6.9 pKd 56
⤷ pKd 6.9 [56]
d[D-Phe2]AVP Peptide Click here for species-specific activity table Hs Full agonist 9.2 pKi 21
⤷ pKi 9.2 [21]
vasopressin {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 8.5 – 9.3 pKi 1,16,20-21,51,56,60,71-72,79,81,87
⤷ pKi 8.5 – 9.3 [1,16,20-21,51,56,60,71-72,79,81,87]
LVP {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 8.6 pKi 81
⤷ pKi 8.6 [81]
arginine vasotocin Peptide Rn Full agonist 8.5 pKi 17
⤷ pKi 8.5 [17]
vasopressin {Sp: Human, Mouse, Rat} Peptide Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Rn Full agonist 8.4 pKi 17
⤷ pKi 8.4 [17]
dAVP Peptide Click here for species-specific activity table Hs Full agonist 8.4 pKi 16,21
⤷ pKi 8.4 [16,21]
arginine vasotocin Peptide Click here for species-specific activity table Hs Full agonist 8.3 pKi 81
⤷ pKi 8.3 [81]
dVDAVP Peptide Click here for species-specific activity table Hs Full agonist 7.6 – 8.0 pKi 21,81
⤷ pKi 7.6 – 8.0 [21,81]
oxytocin {Sp: Human, Mouse, Rat} Peptide Approved drug Click here for species-specific activity table Ligand is endogenous in the given species Hs Full agonist 6.9 – 8.3 pKi 1,18,56,60,71-72,79,81
⤷ pKi 6.9 – 8.3 [1,18,56,60,71-72,79,81]
[Val4]AVP Peptide Click here for species-specific activity table Hs Full agonist 7.5 pKi 21
⤷ pKi 7.5 [21]
d[Leu4]AVP Peptide Click here for species-specific activity table Hs Full agonist 7.4 pKi 16
⤷ pKi 7.4 [16]
desmopressin Peptide Approved drug Click here for species-specific activity table Hs Full agonist 7.0 – 7.7 pKi 16,51,56,60,72,81
⤷ pKi 7.0 – 7.7 [16,51,56,60,72,81]
d[Cha4]AVP Peptide Click here for species-specific activity table Hs Full agonist 7.1 pKi 21
⤷ pKi 7.1 [21]
[Thr4,Gly7]OT Peptide Click here for species-specific activity table Hs Full agonist 6.5 – 6.8 pKi 56,72
⤷ pKi 6.5 – 6.8 [56,72]
[Phe3]OT Peptide Rn Full agonist 6.3 pKi 17
⤷ pKi 6.3 [17]
DAVP Peptide Click here for species-specific activity table Rn Full agonist 6.1 pKi 17
⤷ pKi 6.1 [17]
OPC-51803 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 6.1 pKi 51
⤷ pKi 6.1 [51]
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 6.1 pKi 17
⤷ pKi 6.1 [17]
LIT-001 Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.9 pKi 24
⤷ pKi 5.9 (Ki 1.253x10-6 M) [24]
Description: Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V1a receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
desmopressin Peptide Approved drug Click here for species-specific activity table Rn Full agonist 5.6 pKi 17
⤷ pKi 5.6 [17]
d[Leu4,Dap8]VP Peptide Click here for species-specific activity table Rn Full agonist 5.5 pKi 55
⤷ pKi 5.5 [55]
d[Cha4,Dab8]VP Peptide Click here for species-specific activity table Rn Full agonist 5.4 pKi 55
⤷ pKi 5.4 [55]
d[Leu4]LVP Peptide Click here for species-specific activity table Rn Full agonist 5.4 pKi 55
⤷ pKi 5.4 [55]
d[Cha4]LVP Peptide Click here for species-specific activity table Rn Full agonist 5.0 pKi 55
⤷ pKi 5.0 [55]
selepressin Peptide Hs Full agonist 8.6 pEC50 41
⤷ pEC50 8.6 (EC50 2.4x10-9 M) [41]
View species-specific agonist tables
Agonist Comments
The binding affinities at the V1A receptor found in study [55] are from native tissues.
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Value Parameter Reference
[125I]OH-LVA Peptide Ligand is labelled Ligand is radioactive Hs Antagonist 10.3 – 10.4 pKd 17,20
⤷ pKd 10.3 – 10.4 (Kd 5x10-11 – 3.99x10-11 M) [17,20]
[125I]3-N3-Phpa-LVA Peptide Ligand is labelled Ligand is radioactive Hs Antagonist 9.9 pKd 56
⤷ pKd 9.9 [56]
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 9.3 pKd 9
⤷ pKd 9.3 [9]
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 9.0 pKd 9
⤷ pKd 9.0 [9]
balovaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.6 pKd 61
⤷ pKd 8.6 (Kd 2.56x10-9 M) [61]
[3H]relcovaptan Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Antagonist 8.5 pKd 64
⤷ pKd 8.5 (Kd 2.95x10-9 M) [64]
3-N3-Phpa-LVA Peptide Hs Antagonist 9.6 pKi 56
⤷ pKi 9.6 [56]
SRX246 Small molecule or natural product Hs Antagonist 9.5 pKi 28
⤷ pKi 9.5 (Ki 3x10-10 M) [28]
YM 218 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.5 pKi 75
⤷ pKi 9.5 [75]
OH-LVA Peptide Click here for species-specific activity table Hs Antagonist 9.3 pKi 81
⤷ pKi 9.3 [81]
YM 471 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.2 pKi 84
⤷ pKi 9.2 [84]
[Phaa1,D-Tyr2,Val4,Arg6,Arg-NH29]AVP Peptide Click here for species-specific activity table Hs Antagonist 9.2 pKi 81
⤷ pKi 9.2 [81]
[Phaa1,D-Tyr(Me)2,Arg6,Tyr-NH29]AVP Peptide Click here for species-specific activity table Hs Antagonist 9.1 pKi 81
⤷ pKi 9.1 [81]
[tBaa1,D-Tyr(Et)2,Val4,Lys6,Arg-NH28,des-Gly9]AVP Peptide Click here for species-specific activity table Hs Antagonist 9.1 pKi 81
⤷ pKi 9.1 [81]
d(CH2)5[D-Tyr(Et)2,Val4,Tyr-NH29]AVP Peptide Click here for species-specific activity table Hs Antagonist 9.1 pKi 20
⤷ pKi 9.1 [20]
d(CH2)5[Tyr(Et)2,Val4,des-Gly9]AVP Peptide Click here for species-specific activity table Hs Antagonist 9.1 pKi 72
⤷ pKi 9.1 [72]
d[Pen1,Tyr(Me)2]AVP Peptide Click here for species-specific activity table Hs Antagonist 9.1 pKi 72
⤷ pKi 9.1 [72]
[Phaa1,D-Tyr(Et)2,Lys6,des-Gly9]AVP Peptide Click here for species-specific activity table Hs Antagonist 8.9 – 9.1 pKi 79,81
⤷ pKi 8.9 – 9.1 [79,81]
Ro5028442 Small molecule or natural product Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.0 pKi 58
⤷ pKi 9.0 (Ki 1x10-9 M) [58]
d(CH2)5[Tyr(Me)2,Thr4,Phe(3I,4N3)-NH29]OVT Peptide Click here for species-specific activity table Hs Antagonist 8.9 pKi 9
⤷ pKi 8.9 [9]
d(CH2)5[Tyr(Me)2]AVP Peptide Click here for species-specific activity table Hs Antagonist 8.4 – 9.2 pKi 20,56,60,71-72,81
⤷ pKi 8.4 – 9.2 [20,56,60,71-72,81]
relcovaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.1 – 9.3 pKi 1,20,27,72,79
⤷ pKi 8.1 – 9.3 [1,20,27,72,79]
[Phaa1,D-Tyr(Et)2,Val4,Lys6,Tyr-NH28,des-Gly9]AVP Peptide Click here for species-specific activity table Hs Antagonist 8.5 – 8.6 pKi 79,81
⤷ pKi 8.5 – 8.6 [79,81]
atosiban Peptide Approved drug Click here for species-specific activity table Hs Antagonist 8.3 – 8.5 pKi 1,18,45,65
⤷ pKi 8.3 – 8.5 [1,18,45,65]
d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT Peptide Click here for species-specific activity table Hs Antagonist 8.3 – 8.4 pKi 45,81
⤷ pKi 8.3 – 8.4 [45,81]
conivaptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 8.2 – 8.4 pKi 71-72
⤷ pKi 8.2 – 8.4 [71-72]
d(CH2)5[Tyr(Me)2,Thr4]OVT Peptide Click here for species-specific activity table Hs Antagonist 8.1 pKi 81
⤷ pKi 8.1 [81]
d[D-Pal2]AVP Peptide Click here for species-specific activity table Hs Antagonist 7.5 – 8.4 pKi 21,62,81
⤷ pKi 7.5 – 8.4 (Ki 3.42x10-8 – 4.28x10-9 M) [21,62,81]
tolvaptan Small molecule or natural product Approved drug Click here for species-specific activity table Hs Antagonist 7.9 pKi 87
⤷ pKi 7.9 [87]
RWJ-351647 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.6 pKi 30
⤷ pKi 7.6 [30]
d(CH2)5[D-Ile2,Ile4,Ala-NH29]AVP Peptide Click here for species-specific activity table Hs Antagonist 7.5 pKi 81
⤷ pKi 7.5 [81]
L023103 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.4 pKi 57
⤷ pKi 7.4 [57]
d(CH2)5[D-Ile2,Ile4,Ala-NH2]AVP Peptide Click here for species-specific activity table Hs Antagonist 7.2 – 7.3 pKi 79,81
⤷ pKi 7.2 – 7.3 [79,81]
nelivaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 7.0 pKi 67
⤷ pKi 7.0 [67]
mozavaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 – 7.1 pKi 72,81,87
⤷ pKi 6.8 – 7.1 [72,81,87]
SSR126768A Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.8 pKi 65
⤷ pKi 6.8 [65]
LS-192629 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.7 pKi 18
⤷ pKi 6.7 [18]
satavaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.5 pKi 72,84
⤷ pKi 6.5 [72,84]
tolvaptan Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 6.5 pKi 87
⤷ pKi 6.5 [87]
mozavaptan Small molecule or natural product Click here for species-specific activity table Rn Antagonist 6.3 pKi 87
⤷ pKi 6.3 [87]
OPC-21268 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.1 pKi 81
⤷ pKi 5.1 [81]
View species-specific antagonist tables
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
References:  63
Tissue Distribution Click here for help
Liver > heart, kidney, skeletal muscle.
Species:  Human
Technique:  Northern blotting.
References:  80
Myometrium.
Species:  Human
Technique:  in situ hybridisation.
References:  82
Adrenal gland (medulla and cortex).
Species:  Human
Technique:  RT-PCR.
References:  26,29
Platelets.
Species:  Human
Technique:  RT-PCR.
References:  32
Kidney: glomerulus, initial cortical collecting duct, cortical collecting duct, outer medullary collecting duct, inner medullary collecting duct, arcuate artery > proximal convoluted and straight tubules, inner medullary thin limbs, medullary thick ascending limbs.
Species:  Rat
Technique:  RT-PCR.
References:  76
Uterus.
Species:  Rat
Technique:  RT-PCR.
References:  19
Liver.
Species:  Rat
Technique:  in situ hybridisation.
References:  54
Adrenal gland.
Species:  Rat
Technique:  RT-PCR.
References:  29,83
CNS: frontal cortex, piriform cortex, internal granular layer and the medial, dorsal, ventral and lateral portion of the anterior olfactory nucleus, zona limitans of the islands of Calleja, suprachiasmatic nucleus, CA1, CA2, CA3 and dentate gyrus of the hippocampus, paraventricular hypothalamic nucleus, ventromedial hypothalamic nucleus, arcuate nucleus, lateral habenular nucleus, molecular and granular cell layers of the cerebellum.
Species:  Rat
Technique:  in situ hybridisation.
References:  53,69
Lung.
Species:  Rat
Technique:  Radioligand binding.
References:  74
Testis.
Species:  Rat
Technique:  Radioligand binding.
References:  46
Vascular smooth muscle cells.
Species:  Rat
Technique:  Northern blotting.
References:  49
Cardiomyocytes.
Species:  Rat
Technique:  RT-PCR.
References:  13
Kidney.
Species:  Rat
Technique:  in situ hybridisation.
References:  54
Adult: brain, lung, liver, kidney.
Newborn: brain, liver, heart, kidney.
Species:  Rat
Technique:  RT-PCR.
References:  33
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 human V1A receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of IP accumulation.
References:  79
Measurement of calcium levels in CHO cells transfected with the rat V1A receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Stimulation of calcium mobilisation.
References:  10
Measurement of arachidonic acid levels in CHO cells transfected with the rat V1A receptor.
Species:  Rat
Tissue:  CHO cells.
Response measured:  Stimulation arachidonic acid release.
References:  10
Measurement of calcium levels in CHO cells transfected with the human V1A receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of calcium mobilisation.
References:  72
Measurement of MAP kinase activation in CHO cells transfected with the human V1A receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of MAP kinase activation.
References:  73
Measurement of inositol phosphate accumulation in COS-7 cells transfected with the human V1A receptor.
Species:  Human
Tissue:  COS-7 cells.
Response measured:  Stimulation of IP accumulation.
References:  79
Physiological Functions Click here for help
Glucose homeostasis.
Species:  Mouse
Tissue:  In vivo.
References:  3
Regulation of heart rate.
Species:  Mouse
Tissue:  In vivo.
References:  52
Vasoconstriction.
Species:  Rat
Tissue:  Isolated uterine resistance arteries.
References:  15
Vasoconstriction.
Species:  Rat
Tissue:  Isolated perfused kidney.
References:  44
Vasoconstriction.
Species:  Rat
Tissue:  Isolated mesenteric artery rings.
References:  68
Vasoconstriction.
Species:  Human
Tissue:  In vivo.
References:  11
Hypertension.
Species:  Rat
Tissue:  In vivo.
References:  50,70
Tissue regeneration.
Species:  Rat
Tissue:  Adrenal gland.
References:  83
Aldosterone and corticosterone secretion.
Species:  Rat
Tissue:  Adrenal gland.
References:  25
Platelet aggregation.
Species:  Human
Tissue:  Platelets.
References:  32,66
Cardiomyocyte hypertrophy.
Species:  Mouse
Tissue:  Isolated cardiomyocytes.
References:  36
Myometrial contraction.
Species:  Human
Tissue:  Myometrial strips.
References:  82
Physiological Consequences of Altering Gene Expression Click here for help
V1A receptor knockout mice exhibit impaired spatial memory.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  22
V1A receptor (and V1B receptor) knockout mice exhibit normal, acute intoxicating behavioural effects following ethanol ingestion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  12
V1A receptor knockout mice exhibit impaired aldosterone secretion.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  8
V1A receptor knockout mice exhibit subtle olfactory deficit but normal aggression.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  86
V1A receptor knockout mice exhibit a decrease in blood pressure and circulating blood volume.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  40
V1A receptor knockout mice exhibit altered reflex changes in heart rate.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  52
V1A receptor knockout mice exhibit altered lipid metabolism.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  34
V1A receptor knockout mice exhibit altered glucose homeostasis.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  3
V1A receptor knockout mice exhibit attenuated cardiac hypertrophy in response to pressure overload.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  36
Male V1A receptor knockout mice exhibit a decrease in anxiety-like behaviour and impaired social recognition. No such effects were observed in female V1A knockout mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  6-7
Re-expressing the V1A receptor in the lateral septum of V1A receptor knockout mice restores impaired social memory; mice overexpressing the V1A receptor exhibit potentiation of social recognition and a slight increase in anxiety-related behaviour.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells; viral gene transfer.
References:  5
V1A receptor knockout mice exhibit a decrease in anxiety-like behaviour and impaired social recognition. This effect was seen in both male and female receptor knockout mice suggesting that there is no sexual dimorphism involved.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  23
V1A receptor knockout mice exhibit enhanced proteolysis and gluconeogenesis.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  35
V1A receptor knockout mice (neonatal females) exhibit an orientating bias for familial odours
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells
References:  31
V1A receptor knockout mice exhibit reduced brain edema and secondary damage following traumatic brain injury.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells
References:  59
V1a receptor transgenic mice exhibit altered brain receptor expression and social behaviour
Species:  Mouse
Tissue: 
Technique:  Humanised V1A receptor construct injected into fertilised eggs
References:  14
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
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: 129/Sv * C57BL/6J		 MGI:1859216  MP:0000639 abnormal adrenal gland morphology PMID: 16682631 
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: 129/Sv * C57BL/6J		 MGI:1859216  MP:0004184 abnormal baroreceptor physiology PMID: 16682631 
Avpr1atm1Sbhu Avpr1atm1Sbhu/Avpr1atm1Sbhu
involves: C57BL/6		 MGI:1859216  MP:0002144 abnormal B cell differentiation PMID: 12576226 
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: 129/Sv * C57BL/6J		 MGI:1859216  MP:0005345 abnormal circulating corticosterone level PMID: 16682631 
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: 129/Sv * C57BL/6J		 MGI:1859216  MP:0001629 abnormal heart rate PMID: 16682631 
Avpr1atm1Sbhu Avpr1atm1Sbhu/Avpr1atm1Sbhu
involves: C57BL/6		 MGI:1859216  MP:0002490 abnormal immunoglobulin level PMID: 12576226 
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: C57BL/6		 MGI:1859216  MP:0001449 abnormal learning/ memory PMID: 15036628 
Avpr1atm1Sbhu Avpr1atm1Sbhu/Avpr1atm1Sbhu
129X1.Cg-Avpr1a		 MGI:1859216  MP:0001360 abnormal social investigation PMID: 14647484 
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: 129/Sv * C57BL/6J		 MGI:1859216  MP:0000250 abnormal vasoconstriction PMID: 16682631 
Avpr1atm1Sbhu Avpr1atm1Sbhu/Avpr1atm1Sbhu
129X1.Cg-Avpr1a		 MGI:1859216  MP:0001364 decreased anxiety-related response PMID: 14647484  16046007 
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: 129/Sv * C57BL/6J		 MGI:1859216  MP:0005523 decreased circulating atrial natriuretic factor PMID: 16682631 
Avpr1atm1Sbhu Avpr1atm1Sbhu/Avpr1atm1Sbhu
involves: C57BL/6		 MGI:1859216  MP:0008497 decreased IgG2b level PMID: 12576226 
Avpr1atm1Dgen Avpr1atm1Dgen/Avpr1atm1Dgen
involves: 129P2/OlaHsd * C57BL/6		 MGI:1859216  MP:0009142 decreased prepulse inhibition
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: 129/Sv * C57BL/6J		 MGI:1859216  MP:0001596 hypotension PMID: 16682631 
Avpr1atm1Sbhu Avpr1atm1Sbhu/Avpr1atm1Sbhu
involves: C57BL/6		 MGI:1859216  MP:0008167 increased B-1a cell number PMID: 12576226 
Avpr1atm1Sbhu Avpr1atm1Sbhu/Avpr1atm1Sbhu
involves: C57BL/6		 MGI:1859216  MP:0008500 increased IgG2a level PMID: 12576226 
Avpr1atm1Gzt Avpr1atm1Gzt/Avpr1atm1Gzt
involves: 129/Sv * C57BL/6J		 MGI:1859216  MP:0001633 poor circulation PMID: 16682631 
Biologically Significant Variants Click here for help
Type:  Single nucleotide polymorphisms
Species:  Human
Description:  Four SNPs in the promotor region of the V1A receptor gene have been found in human platelets.
References:  32
General Comments
V1A vasopressin receptors modulate the vasopressor actions of arginine vasopressin (AVP). They have been shown to be present in many tissues including the brain. They mediate vascular smooth muscle cell contraction and proliferation, liver glycogenolysis, platelet aggregation, aldosterone secretion by the adrenals, and subserve neurotransmitter-like actions of AVP in the central nervous system.

Overexpression of the V1A receptor has been found in adrenocorticotropin-independent macromodular adrenal hyperplasia [48,85]. Vasopressin V1A receptors form homodimers in vitro and may heterodimerise with vasopressin V2 and oxytocin receptors [77-78].

The pattern of V1A receptor expression in the brain may be associated with species-typical social behaviours (e.g., affiliative behaviour) in rodents [43,89]. Polymorphisms in the promoter region of the V1A receptor gene have been associated with pre-pulse inhibition [42], decision making in a dictator game [39] and creative dance performance [4] in humans. An association between polymorphisms in the V1A receptor gene and autism has been found in some [88] but not all [38] studies.

References

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1. 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]

2. Andrés M, Trueba M, Guillon G. (2002) Pharmacological characterization of F-180: a selective human V(1a) vasopressin receptor agonist of high affinity. Br J Pharmacol, 135 (7): 1828-36. [PMID:11934825]

3. Aoyagi T, Birumachi J, Hiroyama M, Fujiwara Y, Sanbe A, Yamauchi J, Tanoue A. (2007) Alteration of glucose homeostasis in V1a vasopressin receptor-deficient mice. Endocrinology, 148 (5): 2075-84. [PMID:17303660]

4. Bachner-Melman R, Dina C, Zohar AH, Constantini N, Lerer E, Hoch S, Sella S, Nemanov L, Gritsenko I, Lichtenberg P et al.. (2005) AVPR1a and SLC6A4 gene polymorphisms are associated with creative dance performance. PLoS Genet, 1 (3): e42. [PMID:16205790]

5. Bielsky IF, Hu SB, Ren X, Terwilliger EF, Young LJ. (2005) The V1a vasopressin receptor is necessary and sufficient for normal social recognition: a gene replacement study. Neuron, 47: 503-513. [PMID:16102534]

6. Bielsky IF, Hu SB, Szegda KL, Westphal H, Young LJ. (2004) Profound impairment in social recognition and reduction in anxiety-like behavior in vasopressin V1a receptor knockout mice. Neuropsychopharmacology, 29 (3): 483-93. [PMID:14647484]

7. Bielsky IF, Hu SB, Young LJ. (2005) Sexual dimorphism in the vasopressin system: lack of an altered behavioral phenotype in female V1a receptor knockout mice. Behav Brain Res, 164 (1): 132-6. [PMID:16046007]

8. Birumachi J, Hiroyama M, Fujiwara Y, Aoyagi T, Sanbe A, Tanoue A. (2007) Impaired arginine-vasopressin-induced aldosterone release from adrenal gland cells in mice lacking the vasopressin V1A receptor. Eur J Pharmacol, 566 (1-3): 226-30. [PMID:17449028]

9. Breton C, Chellil H, Kabbaj-Benmansour M, Carnazzi E, Seyer R, Phalipou S, Morin D, Durroux T, Zingg H, Barberis C et al.. (2001) Direct identification of human oxytocin receptor-binding domains using a photoactivatable cyclic peptide antagonist: comparison with the human V1a vasopressin receptor. J Biol Chem, 276 (29): 26931-41. [PMID:11337500]

10. Briley EM, Lolait SJ, Axelrod J, Felder CC. (1994) The cloned vasopressin V1a receptor stimulates phospholipase A2, phospholipase C, and phospholipase D through activation of receptor-operated calcium channels. Neuropeptides, 27 (1): 63-74. [PMID:7969820]

11. Brouard R, Laporte V, Serradeil Le Gal C, Pignol R, Jang H, Donat F, Lockwood G, Fournie D, Dreux F. (1998) Safety, tolerability, and pharmacokinetics of SR 49059, a V1a vasopressin receptor antagonist, after repeated oral administration in healthy volunteers. Adv Exp Med Biol, 449: 455-65. [PMID:10026839]

12. Caldwell HK, Stewart J, Wiedholz LM, Millstein RA, Iacangelo A, Holmes A, Young 3rd WS, Wersinger SR. (2006) The acute intoxicating effects of ethanol are not dependent on the vasopressin 1a or 1b receptors. Neuropeptides, 40 (5): 325-37. [PMID:17049983]

13. Chandrashekhar Y, Prahash AJ, Sen S, Gupta S, Roy S, Anand IS. (2003) The role of arginine vasopressin and its receptors in the normal and failing rat heart. J Mol Cell Cardiol, 35 (5): 495-504. [PMID:12738231]

14. Charles R, Sakurai T, Takahashi N, Elder GA, Gama Sosa MA, Young LJ, Buxbaum JD. (2014) Introduction of the human AVPR1A gene substantially alters brain receptor expression patterns and enhances aspects of social behavior in transgenic mice. Dis Model Mech, 7 (8): 1013-22. [PMID:24924430]

15. Chen YL, Shepherd C, Spinelli W, Lai FM. (1999) Oxytocin and vasopressin constrict rat isolated uterine resistance arteries by activating vasopressin V1A receptors. Eur J Pharmacol, 376: 45-51. [PMID:10440088]

16. Cheng LL, Stoev S, Manning M, Derick S, Pena A, Mimoun MB, Guillon G. (2004) Design of potent and selective agonists for the human vasopressin V1b receptor based on modifications of [deamino-cys1]arginine vasopressin at position 4. J Med Chem, 47: 2375-2388. [PMID:15084136]

17. Chini B, Mouillac B, Ala Y, Balestre MN, Trumpp-Kallmeyer S, Hoflack J, Elands J, Hibert M, Manning M, Jard S et al.. (1995) Tyr115 is the key residue for determining agonist selectivity in the V1a vasopressin receptor. EMBO J, 14 (10): 2176-82. [PMID:7774575]

18. Cirillo R, Gillio Tos E, Schwarz MK, Quattropani A, Scheer A, Missotten M, Dorbais J, Nichols A, Borrelli F, Giachetti C et al.. (2003) Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor. J Pharmacol Exp Ther, 306 (1): 253-61. [PMID:12660315]

19. Clerget MS, Elalouf JM, Germain G. (1997) Quantitative reverse transcription and polymerase chain reaction analysis of oxytocin and vasopressin receptor mRNAs in the rat uterus near parturition. Mol Cell Endocrinol, 136 (1): 79-89. [PMID:9510070]

20. Cotte N, Balestre MN, Aumelas A, Mahé E, Phalipou S, Morin D, Hibert M, Manning M, Durroux T, Barberis C et al.. (2000) Conserved aromatic residues in the transmembrane region VI of the V1a vasopressin receptor differentiate agonist vs. antagonist ligand binding. Eur J Biochem, 267 (13): 4253-63. [PMID:10866830]

21. Derick S, Cheng LL, Voirol MJ, Stoev S, Giacomini M, Wo NC, Szeto HH, Ben Mimoun M, Andres M, Gaillard RC et al.. (2002) [1-deamino-4-cyclohexylalanine] arginine vasopressin: a potent and specific agonist for vasopressin V1b receptors. Endocrinology, 143 (12): 4655-64. [PMID:12446593]

22. Egashira N, Tanoue A, Higashihara F, Mishima K, Fukue Y, Takano Y, Tsujimoto G, Iwasaki K, Fujiwara M. (2004) V1a receptor knockout mice exhibit impairment of spatial memory in an eight-arm radial maze. Neurosci Lett, 356 (3): 195-8. [PMID:15036628]

23. Egashira N, Tanoue A, Matsuda T, Koushi E, Harada S, Takano Y, Tsujimoto G, Mishima K, Iwasaki K, Fujiwara M. (2007) Impaired social interaction and reduced anxiety-related behavior in vasopressin V1a receptor knockout mice. Behav Brain Res, 178 (1): 123-7. [PMID:17227684]

24. Frantz MC, Pellissier LP, Pflimlin E, Loison S, Gandía J, Marsol C, Durroux T, Mouillac B, Becker JAJ, Le Merrer J et al.. (2018) LIT-001, the First Nonpeptide Oxytocin Receptor Agonist that Improves Social Interaction in a Mouse Model of Autism. J Med Chem, 61 (19): 8670-8692. [PMID:30199637]

25. Grazzini E, Boccara G, Joubert D, Trueba M, Durroux T, Guillon G, Gallo-Payet N, Chouinard L, Payet MD, Serradeil Le Gal C. (1998) Vasopressin regulates adrenal functions by acting through different vasopressin receptor subtypes. Adv Exp Med Biol, 449: 325-34. [PMID:10026821]

26. Grazzini E, Breton C, Derick S, Andres M, Raufaste D, Rickwaert F, Boccara G, Colson P, Guérineau NC, Serradeil-le Gal C et al.. (1999) Vasopressin receptors in human adrenal medulla and pheochromocytoma. J Clin Endocrinol Metab, 84 (6): 2195-203. [PMID:10372731]

27. Griffante C, Green A, Curcuruto O, Haslam CP, Dickinson BA, Arban R. (2005) Selectivity of d[Cha4]AVP and SSR149415 at human vasopressin and oxytocin receptors: evidence that SSR149415 is a mixed vasopressin V1b/oxytocin receptor antagonist. Br J Pharmacol, 146: 744-751. [PMID:16158071]

28. Guillon CD, Koppel GA, Brownstein MJ, Chaney MO, Ferris CF, Lu SF, Fabio KM, Miller MJ, Heindel ND, Hunden DC et al.. (2007) Azetidinones as vasopressin V1a antagonists. Bioorg Med Chem, 15 (5): 2054-80. [PMID:17234419]

29. Guillon G, Grazzini E, Andrez M, Breton C, Trueba M, Serradeil-LeGal C, Boccara G, Derick S, Chouinard L, Gallo-Payet N. (1998) Vasopressin : a potent autocrine/paracrine regulator of mammal adrenal functions. Endocr Res, 24 (3-4): 703-10. [PMID:9888562]

30. Gunnet JW, Matthews JM, Maryanoff BE, de Garavilla L, Andrade-Gordon P, Damiano B, Hageman W, Look R, Stahle P, Streeter AJ et al.. (2006) Characterization of RWJ-351647, a novel nonpeptide vasopressin V2 receptor antagonist. Clin Exp Pharmacol Physiol, 33 (4): 320-6. [PMID:16620295]

31. Hammock EA, Law CS, Levitt P. (2013) Vasopressin eliminates the expression of familiar odor bias in neonatal female mice through V1aR. Horm Behav, 63 (2): 352-60. [PMID:23261858]

32. Hasan KN, Shoji M, Tsutaya S, Kudo R, Matsuda E, Saito J, Kimura T, Yasujima M. (2006) Study of V1a vasopressin receptor gene single nucleotide polymorphisms in platelet vasopressin responsiveness. J Clin Lab Anal, 20 (3): 87-92. [PMID:16721832]

33. Hirasawa A, Hashimoto K, Tsujimoto G. (1994) Distribution and developmental change of vasopressin V1A and V2 receptor mRNA in rats. Eur J Pharmacol, 267 (1): 71-5. [PMID:8206132]

34. Hiroyama M, Aoyagi T, Fujiwara Y, Birumachi J, Shigematsu Y, Kiwaki K, Tasaki R, Endo F, Tanoue A. (2007) Hypermetabolism of fat in V1a vasopressin receptor knockout mice. Mol Endocrinol, 21: 247-258. [PMID:17021052]

35. Hiroyama M, Aoyagi T, Fujiwara Y, Oshikawa S, Sanbe A, Endo F, Tanoue A. (2007) Hyperammonaemia in V1a vasopressin receptor knockout mice caused by the promoted proteolysis and reduced intrahepatic blood volume. J Physiol (Lond.), 581 (Pt 3): 1183-92. [PMID:17379633]

36. Hiroyama M, Wang S, Aoyagi T, Oikawa R, Sanbe A, Takeo S, Tanoue A. (2007) Vasopressin promotes cardiomyocyte hypertrophy via the vasopressin V1A receptor in neonatal mice. Eur J Pharmacol, 559 (2-3): 89-97. [PMID:17275806]

37. Kikuchi S, Tanoue A, Goda N, Matsuo N, Tsujimoto G. (1999) Structure and sequence of the mouse V1a and V1b vasopressin receptor genes. Jpn J Pharmacol, 81: 388-392. [PMID:10669045]

38. Kim SJ, Young LJ, Gonen D, Veenstra-VanderWeele J, Courchesne R, Courchesne E, Lord C, Leventhal BL, Cook Jr EH, Insel TR. (2002) Transmission disequilibrium testing of arginine vasopressin receptor 1A (AVPR1A) polymorphisms in autism. Mol Psychiatry, 7 (5): 503-7. [PMID:12082568]

39. Knafo A, Israel S, Darvasi A, Bachner-Melman R, Uzefovsky F, Cohen L, Feldman E, Lerer E, Laiba E, Raz Y et al.. (2008) Individual differences in allocation of funds in the dictator game associated with length of the arginine vasopressin 1a receptor RS3 promoter region and correlation between RS3 length and hippocampal mRNA. Genes Brain Behav, 7 (3): 266-75. [PMID:17696996]

40. Koshimizu TA, Nasa Y, Tanoue A, Oikawa R, Kawahara Y, Kiyono Y, Adachi T, Tanaka T, Kuwaki T, Mori T et al.. (2006) V1a vasopressin receptors maintain normal blood pressure by regulating circulating blood volume and baroreflex sensitivity. Proc Natl Acad Sci USA, 103 (20): 7807-12. [PMID:16682631]

41. Laporte R, Kohan A, Heitzmann J, Wisniewska H, Toy J, La E, Tariga H, Alagarsamy S, Ly B, Dykert J et al.. (2011) Pharmacological characterization of FE 202158, a novel, potent, selective, and short-acting peptidic vasopressin V1a receptor full agonist for the treatment of vasodilatory hypotension. J Pharmacol Exp Ther, 337 (3): 786-96. [PMID:21411496]

42. Levin R, Heresco-Levy U, Bachner-Melman R, Israel S, Shalev I, Ebstein RP. (2009) Association between arginine vasopressin 1a receptor (AVPR1a) promoter region polymorphisms and prepulse inhibition. Psychoneuroendocrinology, 34 (6): 901-8. [PMID:19195791]

43. Lim MM, Wang Z, Olazábal DE, Ren X, Terwilliger EF, Young LJ. (2004) Enhanced partner preference in a promiscuous species by manipulating the expression of a single gene. Nature, 429 (6993): 754-7. [PMID:15201909]

44. Loichot C, Krieger JP, De Jong W, Nisato D, Imbs JL, Barthelmebs M. (2001) High concentrations of oxytocin cause vasoconstriction by activating vasopressin V1A receptors in the isolated perfused rat kidney. Naunyn Schmiedebergs Arch Pharmacol, 363 (4): 369-75. [PMID:11330329]

45. Manning M, Cheng LL, Stoev S, Wo NC, Chan WY, Szeto HH, Durroux T, Mouillac B, Barberis C. (2005) Design of peptide oxytocin antagonists with strikingly higher affinities and selectivities for the human oxytocin receptor than atosiban. J Pept Sci, 11 (10): 593-608. [PMID:15880385]

46. Meidan R, Hsueh AJ. (1985) Identification and characterization of arginine vasopressin receptors in the rat testis. Endocrinology, 116 (1): 416-23. [PMID:2981073]

47. Morel A, O'Carroll AM, Brownstein MJ, Lolait SJ. (1992) Molecular cloning and expression of a rat V1a arginine vasopressin receptor. Nature, 356 (6369): 523-6. [PMID:1560825]

48. Mune T, Murase H, Yamakita N, Fukuda T, Murayama M, Miura A, Suwa T, Hanafusa J, Daido H, Morita H et al.. (2002) Eutopic overexpression of vasopressin v1a receptor in adrenocorticotropin-independent macronodular adrenal hyperplasia. J Clin Endocrinol Metab, 87 (12): 5706-13. [PMID:12466375]

49. Murasawa S, Matsubara H, Kizima K, Maruyama K, Mori Y, Inada M. (1995) Glucocorticoids regulate V1a vasopressin receptor expression by increasing mRNA stability in vascular smooth muscle cells. Hypertension, 26 (4): 665-9. [PMID:7558228]

50. Naitoh M, Burrell LM, Risvanis J, Aldred KL, Rockell MD, Johnston CI, Phillips PA. (1997) Modulation of genetic hypertension by short-term AVP V1A or V2 receptor antagonism in young SHR. Am J Physiol, 272 (2 Pt 2): F229-34. [PMID:9124400]

51. Nakamura S, Yamamura Y, Itoh S, Hirano T, Tsujimae K, Aoyama M, Kondo K, Ogawa H, Shinohara T, Kan K et al.. (2000) Characterization of a novel nonpeptide vasopressin V(2)-agonist, OPC-51803, in cells transfected human vasopressin receptor subtypes. Br J Pharmacol, 129 (8): 1700-6. [PMID:10780976]

52. Oikawa R, Nasa Y, Ishii R, Kuwaki T, Tanoue A, Tsujimoto G, Takeo S. (2007) Vasopressin V1A receptor enhances baroreflex via the central component of the reflex arc. Eur J Pharmacol, 558 (1-3): 144-50. [PMID:17224142]

53. Ostrowski NL, Lolait SJ, Young 3rd WS. (1994) Cellular localization of vasopressin V1a receptor messenger ribonucleic acid in adult male rat brain, pineal, and brain vasculature. Endocrinology, 135 (4): 1511-28. [PMID:7925112]

54. Ostrowski NL, Young 3rd WS, Knepper MA, Lolait SJ. (1993) Expression of vasopressin V1a and V2 receptor messenger ribonucleic acid in the liver and kidney of embryonic, developing, and adult rats. Endocrinology, 133 (4): 1849-59. [PMID:8404628]

55. Pena A, Murat B, Trueba M, Ventura MA, Wo NC, Szeto HH, Cheng LL, Stoev S, Guillon G, Manning M. (2007) Design and synthesis of the first selective agonists for the rat vasopressin V(1b) receptor: based on modifications of deamino-[Cys1]arginine vasopressin at positions 4 and 8. J Med Chem, 50: 835-847. [PMID:17300166]

56. Phalipou S, Cotte N, Carnazzi E, Seyer R, Mahe E, Jard S, Barberis C, Mouillac B. (1997) Mapping peptide-binding domains of the human V1a vasopressin receptor with a photoactivatable linear peptide antagonist. J Biol Chem, 272 (42): 26536-44. [PMID:9334232]

57. Quattropani A, Dorbais J, Covini D, Pittet PA, Colovray V, Thomas RJ, Coxhead R, Halazy S, Scheer A, Missotten M et al.. (2005) Discovery and development of a new class of potent, selective, orally active oxytocin receptor antagonists. J Med Chem, 48 (24): 7882-905. [PMID:16302826]

58. Ratni H, Rogers-Evans M, Bissantz C, Grundschober C, Moreau JL, Schuler F, Fischer H, Alvarez Sanchez R, Schnider P. (2015) Discovery of highly selective brain-penetrant vasopressin 1a antagonists for the potential treatment of autism via a chemogenomic and scaffold hopping approach. J Med Chem, 58 (5): 2275-89. [PMID:25654260]

59. Rauen K, Trabold R, Brem C, Terpolilli NA, Plesnila N. (2013) Arginine vasopressin V1a receptor-deficient mice have reduced brain edema and secondary brain damage following traumatic brain injury. J Neurotrauma, 30 (16): 1442-8. [PMID:23441636]

60. Saito M, Tahara A, Sugimoto T. (1997) 1-desamino-8-D-arginine vasopressin (DDAVP) as an agonist on V1b vasopressin receptor. Biochem Pharmacol, 53: 1711-1717. [PMID:9264324]

61. Schnider P, Bissantz C, Bruns A, Dolente C, Goetschi E, Jakob-Roetne R, Künnecke B, Mueggler T, Muster W, Parrott N et al.. (2020) Discovery of Balovaptan, a Vasopressin 1a Receptor Antagonist for the Treatment of Autism Spectrum Disorder. J Med Chem, 63 (4): 1511-1525. [PMID:31951127]

62. Schwartz J, Derdowska I, Sobocinska M, Kupryszewski G. (1991) A potent new synthetic analog of vasopressin with relative agonist specificity for the pituitary. Endocrinology, 129 (2): 1107-9. [PMID:1649739]

63. Schöneberg T, Kostenis E, Liu J, Gudermann T, Wess J. (1998) Molecular aspects of vasopressin receptor function. Adv Exp Med Biol, 449: 347-58. [PMID:10026824]

64. Serradeil-Le Gal C, Raufaste D, Marty E, Garcia C, Maffrand JP, Le Fur G. (1994) Binding of [3H] SR 49059, a potent nonpeptide vasopressin V1a antagonist, to rat and human liver membranes. Biochem Biophys Res Commun, 199 (1): 353-60. [PMID:8123034]

65. Serradeil-Le Gal C, Valette G, Foulon L, Germain G, Advenier C, Naline E, Bardou M, Martinolle J-P, Pouzet B, Raufaste D, Garcia C, Double-Cazenave E, Pauly M, Pascal M, Barbier A, Scatton B, Maffrand J-P, Le Fur G. (2004) SSR126768A (4-Chloro-3-[(3R)-(+)-5-chloro-1-(2,4-dimethoxybenzyl)-3-methyl-2oxo-2,3-dihydro-1H-indol-3-yl]-N-ethyl-N-(3-pyridylmethyl)-benzamidine, hydrochloride): a new selective and orally active oxytocin receptor antagonist for the prevention of preterm labor. J Pharmacol Exp Therap, 309: 414-424. [PMID:14722330]

66. Serradeil-Le Gal C, Wagnon J, Garcia C, Lacour C, Guiraudou P, Christophe B, Villanova G, Nisato D, Maffrand JP, Le Fur G et al.. (1993) Biochemical and pharmacological properties of SR49059, a new potent nonpeptide antagonist of rat and human vasopressin V1a receptor. J Clin Invest, 92: 224-231. [PMID:8392086]

67. Serradeil-Le Gal C, Wagnon J, Simiand J, Griebel G, Lacour C, Guillon G, Barberis C, Brossard G, Soubrie P, Nisato D, Pascal M, Pruss R, Scatton B, Maffrand JP, Le Fur G. (2002) Characterization of (2S,4R)-1-[5-chloro-1-[(2,4-dimethoxyphenyl)sulfonyl]-3-(2-methoxy-phenyl)-2-oxo-2,3-dihydro-1H-indol-3-yl]-4-hydroxy-N,N-dimethyl-2-pyrrolidine carboxamide (SSR149415), a selective and orally active vasopressin V1b receptor antagonist. J Pharmacol Exp Ther, 300: 1122-1130. [PMID:11861823]

68. Shi W, Cui N, Shi Y, Zhang X, Yang Y, Jiang C. (2007) Arginine vasopressin inhibits Kir6.1/SUR2B channel and constricts the mesenteric artery via V1a receptor and protein kinase C. Am J Physiol Regul Integr Comp Physiol, 293 (1): R191-9. [PMID:17428891]

69. Szot P, Bale TL, Dorsa DM. (1994) Distribution of messenger RNA for the vasopressin V1a receptor in the CNS of male and female rats. Brain Res Mol Brain Res, 24: 1-10. [PMID:7968346]

70. Tachikawa K, Yokoi H, Nagasaki H, Arima H, Murase T, Sugimura Y, Miura Y, Hirabayashi M, Oiso Y. (2003) Altered cardiovascular regulation in arginine vasopressin-overexpressing transgenic rat. Am J Physiol Endocrinol Metab, 285 (6): E1161-6. [PMID:12915399]

71. Tahara A, Saito M, Sugimoto T, Tomura Y, Wada K, Kusayama T, Tsukada J, Ishii N, Yatsu T, Uchida W et al.. (1998) Pharmacological characterization of YM087, a potent, nonpeptide human vasopressin V1A and V2 receptor antagonist. Naunyn Schmiedebergs Arch Pharmacol, 357 (1): 63-9. [PMID:9459574]

72. Tahara A, Saito M, Sugimoto T, Tomura Y, Wada K, Kusayama T, Tsukada J, Ishii N, Yatsu T, Uchida W et al.. (1998) Pharmacological characterization of the human vasopressin receptor subtypes stably expressed in Chinese hamster ovary cells. Br J Pharmacol, 125 (7): 1463-70. [PMID:9884074]

73. Tahara A, Saito M, Sugimoto T, Tomura Y, Wada K, Kusayama T, Tsukada J, Ishii N, Yatsu T, Uchida W et al.. (1999) AVP-induced mitogenic responses of Chinese hamster ovary cells expressing human V1A or V1B receptors. Pflugers Arch, 437 (2): 219-26. [PMID:9929562]

74. Tahara A, Tomura Y, Wada K, Kusayama T, Tsukada J, Ishii N, Yatsu T, Uchida W, Tanaka A. (1998) Characterization of vasopressin receptor in rat lung. Neuropeptides, 32 (3): 281-6. [PMID:10189064]

75. Tahara A, Tsukada J, Tomura Y, Kusayama T, Wada K, Ishii N, Taniguchi N, Suzuki T, Yatsu T, Uchida W et al.. (2005) Effects of YM218, a nonpeptide vasopressin V1A receptor-selective antagonist, on human vasopressin and oxytocin receptors. Pharmacol Res, 51 (3): 275-81. [PMID:15661579]

76. Terada Y, Tomita K, Nonoguchi H, Yang T, Marumo F. (1993) Different localization and regulation of two types of vasopressin receptor messenger RNA in microdissected rat nephron segments using reverse transcription polymerase chain reaction. J Clin Invest, 92 (5): 2339-45. [PMID:8227349]

77. Terrillon S, Barberis C, Bouvier M. (2004) Heterodimerization of V1a and V2 vasopressin receptors determines the interaction with beta-arrestin and their trafficking patterns. Proc Natl Acad Sci USA, 101 (6): 1548-53. [PMID:14757828]

78. Terrillon S, Durroux T, Mouillac B, Breit A, Ayoub MA, Taulan M, Jockers R, Barberis C, Bouvier M. (2003) Oxytocin and vasopressin V1a and V2 receptors form constitutive homo- and heterodimers during biosynthesis. Mol Endocrinol, 17 (4): 677-91. [PMID:12554793]

79. Thibonnier M, Auzan C, Madhun Z, Wilkins P, Berti-Mattera L, Clauser E. (1994) Molecular cloning, sequencing, and functional expression of a cDNA encoding the human V1a vasopressin receptor. J Biol Chem, 269 (5): 3304-10. [PMID:8106369]

80. Thibonnier M, Graves MK, Wagner MS, Auzan C, Clauser E, Willard HF. (1996) Structure, sequence, expression, and chromosomal localization of the human V1a vasopressin receptor gene. Genomics, 31 (3): 327-34. [PMID:8838314]

81. Thibonnier M, Preston JA, Dulin N, Wilkins PL, Berti-Mattera LN, Mattera R. (1997) The human V3 pituitary vasopressin receptor: ligand binding profile and density-dependent signaling pathways. Endocrinology, 138 (10): 4109-22. [PMID:9322919]

82. Thornton S, Baldwin PJ, Harris PA, Harding F, Davison JM, Baylis PH, Timmons PM, Wathes DC. (2002) The role of arginine vasopressin in human labour: functional studies, fetal production and localisation of V1a receptor mRNA. BJOG, 109 (1): 57-62. [PMID:11843375]

83. Trejter M, Carraro G, Rucinski M, Hochol A, Rebuffat P, Nussdorfer GG, Malendowicz LK. (2005) Arginin-vasopressin regulates proliferative activity of the regenerating rat adrenal cortex. Int J Mol Med, 15: 993-997. [PMID:15870905]

84. Tsukada J, Tahara A, Tomura Y, Wada Ki, Kusayama T, Ishii N, Yatsu T, Uchida W, Taniguchi N, Tanaka A. (2001) Effects of YM471, a nonpeptide AVP V(1A) and V(2) receptor antagonist, on human AVP receptor subtypes expressed in CHO cells and oxytocin receptors in human uterine smooth muscle cells. Br J Pharmacol, 133 (5): 746-54. [PMID:11429400]

85. Vezzosi D, Cartier D, Régnier C, Otal P, Bennet A, Parmentier F, Plantavid M, Lacroix A, Lefebvre H, Caron P. (2007) Familial adrenocorticotropin-independent macronodular adrenal hyperplasia with aberrant serotonin and vasopressin adrenal receptors. Eur J Endocrinol, 156 (1): 21-31. [PMID:17218722]

86. Wersinger SR, Caldwell HK, Martinez L, Gold P, Hu SB, Young 3rd WS. (2007) Vasopressin 1a receptor knockout mice have a subtle olfactory deficit but normal aggression. Genes Brain Behav, 6 (6): 540-51. [PMID:17083331]

87. Yamamura Y, Nakamura S, Itoh S, Hirano T, Onogawa T, Yamashita T, Yamada Y, Tsujimae K, Aoyama M, Kotosai K et al.. (1998) OPC-41061, a highly potent human vasopressin V2-receptor antagonist: pharmacological profile and aquaretic effect by single and multiple oral dosing in rats. J Pharmacol Exp Ther, 287 (3): 860-7. [PMID:9864265]

88. Yirmiya N, Rosenberg C, Levi S, Salomon S, Shulman C, Nemanov L, Dina C, Ebstein RP. (2006) Association between the arginine vasopressin 1a receptor (AVPR1a) gene and autism in a family-based study: mediation by socialization skills. Mol Psychiatry, 11 (5): 488-94. [PMID:16520824]

89. Young LJ, Nilsen R, Waymire KG, MacGregor GR, Insel TR. (1999) Increased affiliative response to vasopressin in mice expressing the V1a receptor from a monogamous vole. Nature, 400 (6746): 766-8. [PMID:10466725]

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