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V2 receptor

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Target not currently curated in GtoImmuPdb

Target id: 368

Nomenclature: V2 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 7 371 Xq28 AVPR2 arginine vasopressin receptor 2 8,72
Mouse 7 371 X 37.46 cM Avpr2 arginine vasopressin receptor 2 54
Rat 7 371 Xq37 Avpr2 arginine vasopressin receptor 2 45
Previous and Unofficial Names Click here for help
ADHR | DIR3 | antidiuretic hormone receptor | renal-type arginine vasopressin receptor
Database Links Click here for help
Specialist databases
GPCRdb v2r_human (Hs), v2r_mouse (Mm), v2r_rat (Rn)
Other databases
Alphafold P30518 (Hs), O88721 (Mm), Q00788 (Rn)
ChEMBL Target CHEMBL1790 (Hs), CHEMBL3766 (Rn)
DrugBank Target P30518 (Hs)
Ensembl Gene ENSG00000126895 (Hs), ENSMUSG00000031390 (Mm), ENSRNOG00000059862 (Rn)
Entrez Gene 554 (Hs), 12000 (Mm), 25108 (Rn)
Human Protein Atlas ENSG00000126895 (Hs)
KEGG Gene hsa:554 (Hs), mmu:12000 (Mm), rno:25108 (Rn)
OMIM 304800 (Hs)
Orphanet ORPHA118947 (Hs)
Pharos P30518 (Hs)
RefSeq Nucleotide NM_000054 (Hs), NM_019404 (Mm), NM_019136 (Rn)
RefSeq Protein NP_000045 (Hs), NP_062277 (Mm), NP_062009 (Rn)
UniProtKB P30518 (Hs), O88721 (Mm), Q00788 (Rn)
Wikipedia AVPR2 (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)  [1,11,13,60,74,79,89]

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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 Full agonist 8.4 – 9.4 pKd 17,50,78-79,89
⤷ pKd 8.4 – 9.4 (Kd 3.98x10-9 – 3.99x10-10 M) [17,50,78-79,89]
[3H]AVP (human, mouse, rat) Peptide Ligand is labelled Ligand is radioactive Rn Full agonist 8.8 pKd 17
⤷ pKd 8.8 [17]
[3H]dDAVP Peptide Ligand is labelled Ligand is radioactive Hs Full agonist 7.2 – 9.1 pKd 46
⤷ pKd 7.2 – 9.1 (Kd 6.3x10-8 – 8x10-10 M) [46]
[3H]OT (human, mouse, rat) Peptide Click here for species-specific activity table Ligand is labelled Ligand is radioactive Hs Full agonist 5.8 pKd
⤷ pKd 5.8
dVDAVP Peptide Click here for species-specific activity table Hs Full agonist 8.6 – 9.1 pKi 21,83
⤷ pKi 8.6 – 9.1 [21,83]
desmopressin Peptide Approved drug Click here for species-specific activity table Rn Full agonist 8.7 pKi 17
⤷ pKi 8.7 [17]
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 7.9 – 9.1 pKi 1,11,13,21,50,66,74,78-79,83,89
⤷ pKi 7.9 – 9.1 [1,11,13,21,50,66,74,78-79,83,89]
[Val4]AVP Peptide Click here for species-specific activity table Hs Full agonist 8.4 pKi 21
⤷ pKi 8.4 [21]
DAVP Peptide Click here for species-specific activity table Rn Full agonist 8.3 pKi 17
⤷ pKi 8.3 [17]
dAVP Peptide Click here for species-specific activity table Hs Full agonist 8.3 pKi 11,21
⤷ pKi 8.3 [11,21]
desmopressin Peptide Approved drug Click here for species-specific activity table Hs Full agonist 7.2 – 8.6 pKi 11,13,17,50,66,74,79,83
⤷ pKi 7.2 – 8.6 (Ki 6.3x10-8 – 2.5x10-9 M) [11,13,17,50,66,74,79,83]
arginine vasotocin Peptide Click here for species-specific activity table Hs Full agonist 7.6 – 8.2 pKi 13,83
⤷ pKi 7.6 – 8.2 [13,83]
LVP {Sp: Pig} Peptide Click here for species-specific activity table Hs Full agonist 7.0 – 8.5 pKi 74,83
⤷ pKi 7.0 – 8.5 [74,83]
DAVP Peptide Hs Full agonist 7.3 – 7.6 pKi 13,17
⤷ pKi 7.3 – 7.6 [13,17]
[Phe3]OT Peptide Click here for species-specific activity table Hs Full agonist 7.1 pKi 13
⤷ pKi 7.1 [13]
OPC-51803 Small molecule or natural product Click here for species-specific activity table Hs Full agonist 7.0 pKi 50
⤷ pKi 7.0 [50]
d[Leu4]LVP Peptide Click here for species-specific activity table Rn Full agonist 7.0 pKi 60
⤷ pKi 7.0 [60]
d[D-Phe2]AVP Peptide Click here for species-specific activity table Hs Full agonist 6.6 pKi 21
⤷ pKi 6.6 [21]
d[Leu4,Dap8]VP Peptide Click here for species-specific activity table Rn Full agonist 6.6 pKi 60
⤷ pKi 6.6 [60]
d[Leu4]AVP Peptide Click here for species-specific activity table Hs Full agonist 6.6 pKi 11
⤷ pKi 6.6 [11]
d[Cha4]AVP Peptide Click here for species-specific activity table Hs Full agonist 6.5 pKi 21
⤷ pKi 6.5 [21]
d[Cha4,Dab8]VP Peptide Click here for species-specific activity table Rn Full agonist 6.3 pKi 60
⤷ pKi 6.3 [60]
d[Cha4]LVP Peptide Click here for species-specific activity table Rn Full agonist 6.2 pKi 60
⤷ pKi 6.2 [60]
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 5.4 – 6.8 pKi 13,15,66,78-79,83
⤷ pKi 5.4 – 6.8 [13,15,66,78-79,83]
LIT-001 Small molecule or natural product Click here for species-specific activity table Hs Agonist 5.8 pKi 30
⤷ pKi 5.8 (Ki 1.666x10-6 M) [30]
Description: Binding affinity determined by a TR-FRET binding assay on HEK cells expressing SNAP-tagged V2 receptors using 20 nM fluorescent DY647 and increasing concentration of competitor.
d[D-Pal2]AVP Peptide Click here for species-specific activity table Hs Agonist 5.0 – 5.2 pKi 21,69,83
⤷ pKi 5.0 – 5.2 (Ki 9.6x10-6 – 6.422x10-6 M) [21,69,83]
VNA932 Small molecule or natural product Hs Full agonist 7.1 pIC50 24
⤷ pIC50 7.1 (IC50 8x10-8 M) [24]
View species-specific agonist tables
Agonist Comments
The binding affinities at the V2 receptor found in study [60] 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]d(CH2)5[D-Ile2,Ile4,Tyr-NH29]AVP Peptide Ligand is labelled Ligand is radioactive Rn Antagonist 9.5 pKd 17
⤷ pKd 9.5 [17]
[125I]d(CH2)5[D-Tyr(Et)2,Val4,Tyr-NH29]AVP Peptide Ligand is labelled Ligand is radioactive Rn Antagonist 9.4 pKd 17
⤷ pKd 9.4 [17]
[125I]d(CH2)5[D-Tyr(Et)2,Ile4,Tyr-NH29]AVP Peptide Ligand is labelled Ligand is radioactive Rn Antagonist 9.3 pKd 17
⤷ pKd 9.3 [17]
[125I]d(CH2)5[D-Ile2,Val4,Tyr-NH29]AVP Peptide Ligand is labelled Ligand is radioactive Rn Antagonist 9.2 pKd 17
⤷ pKd 9.2 [17]
[125I]d(CH2)5[D-Tyr(Et)2,Ile4,Tyr-NH29]AVP Peptide Ligand is labelled Ligand is radioactive Hs Antagonist 9.1 pKd 17
⤷ pKd 9.1 [17]
[125I]d(CH2)5[D-Tyr(Et)2,Val4,Tyr-NH29]AVP Peptide Ligand is labelled Ligand is radioactive Hs Antagonist 9.1 pKd 17
⤷ pKd 9.1 [17]
[3H]SR 121463A Small molecule or natural product Ligand is labelled Ligand is radioactive Hs Inverse agonist 8.4 – 9.3 pKd 17,73
⤷ pKd 8.4 – 9.3 (Kd 4.1x10-9 – 5x10-10 M) [17,73]
balovaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.0 pKd 68
⤷ pKd 5.0 (Kd 9.953x10-6 M) [68]
conivaptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.4 pKi 19
⤷ pKi 9.4 (Ki 3.6x10-10 M) [19]
tolvaptan Small molecule or natural product Approved drug Primary target of this compound Click here for species-specific activity table Hs Antagonist 9.4 pKi 89
⤷ pKi 9.4 (Ki 4.3x10-10 M) [89]
satavaptan Small molecule or natural product Rn Antagonist 9.3 pKi 17
⤷ pKi 9.3 [17]
d(CH2)5[D-Tyr(Et)2,Val4,Tyr-NH29]AVP Peptide Click here for species-specific activity table Hs Antagonist 9.1 pKi 16
⤷ pKi 9.1 [16]
lixivaptan Small molecule or natural product Hs Inverse agonist 8.9 – 9.2 pKi 4,74
⤷ pKi 8.9 – 9.2 [4,74]
RWJ-351647 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 9.0 pKi 33
⤷ pKi 9.0 [33]
YM 471 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.9 pKi 84
⤷ pKi 8.9 [84]
tolvaptan Small molecule or natural product Approved drug Click here for species-specific activity table Rn Antagonist 8.9 pKi 89
⤷ pKi 8.9 [89]
SKF-105494 Peptide Hs Antagonist 8.9 pKi 74
⤷ pKi 8.9 [74]
satavaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 8.4 – 9.3 pKi 1,17,73-74,79
⤷ pKi 8.4 – 9.3 [1,17,73-74,79]
d(CH2)5[D-Ile2,Val4,Tyr-NH29]AVP Peptide Rn Antagonist 8.6 pKi 17
⤷ pKi 8.6 [17]
d(CH2)5[D-Ile2,Ile4,Tyr-NH29]AVP Peptide Rn Antagonist 8.4 pKi 17
⤷ pKi 8.4 [17]
d(CH2)5[Tyr(Et)2,Val4,des-Gly9]AVP Peptide Click here for species-specific activity table Hs Antagonist 8.0 – 8.3 pKi 74,79
⤷ pKi 8.0 – 8.3 [74,79]
mozavaptan Small molecule or natural product Click here for species-specific activity table Rn Inverse agonist 7.4 – 8.2 pKi 17,89
⤷ pKi 7.4 – 8.2 [17,89]
mozavaptan Small molecule or natural product Click here for species-specific activity table Hs Inverse agonist 7.4 – 8.1 pKi 17,74,79,83,89
⤷ pKi 7.4 – 8.1 [17,74,79,83,89]
d(CH2)5[D-Ile2,Ile4]AVP Peptide Hs Antagonist 6.9 – 8.4 pKi 17,74
⤷ pKi 6.9 – 8.4 [17,74]
d(CH2)5[D-Ile2,Ile4,Ala-NH29]AVP Peptide Click here for species-specific activity table Hs Antagonist 7.1 – 7.7 pKi 74,83
⤷ pKi 7.1 – 7.7 [74,83]
[tBaa1,D-Tyr(Et)2,Val4,Lys6,Arg-NH28,des-Gly9]AVP Peptide Click here for species-specific activity table Hs Antagonist 7.3 pKi 83
⤷ pKi 7.3 [83]
d(CH2)5[D-Ile2,Val4,Tyr-NH29]AVP Peptide Hs Antagonist 7.3 pKi 17
⤷ pKi 7.3 [17]
d(CH2)5[D-Ile2,Ile4,Ala-NH2]AVP Peptide Click here for species-specific activity table Hs Antagonist 7.1 pKi 83
⤷ pKi 7.1 [83]
d(CH2)5[D-Ile2,Ile4,Tyr-NH29]AVP Peptide Hs Antagonist 6.9 pKi 17
⤷ pKi 6.9 [17]
d(CH2)5[Tyr(Me)2]AVP Peptide Click here for species-specific activity table Hs Antagonist 6.7 – 7.1 pKi 16,66,74,78-79,83
⤷ pKi 6.7 – 7.1 [16,66,74,78-79,83]
relcovaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.6 – 6.9 pKi 16,74,79,83-84
⤷ pKi 6.6 – 6.9 [16,74,79,83-84]
d(CH2)5[Tyr(Me)2,Thr4,Phe(3I,4N3)-NH29]OVT Peptide Click here for species-specific activity table Hs Antagonist 6.7 pKi 9
⤷ pKi 6.7 [9]
[Phaa1,D-Tyr2,Val4,Arg6,Arg-NH29]AVP Peptide Click here for species-specific activity table Hs Antagonist 6.6 pKi 83
⤷ pKi 6.6 [83]
[Phaa1,D-Tyr(Et)2,Lys6,des-Gly9]AVP Peptide Click here for species-specific activity table Hs Antagonist 6.5 – 6.6 pKi 74,83
⤷ pKi 6.5 – 6.6 [74,83]
d[Pen1,Tyr(Me)2]AVP Peptide Click here for species-specific activity table Hs Antagonist 6.4 – 6.7 pKi 74,79
⤷ pKi 6.4 – 6.7 [74,79]
[Phaa1,D-Tyr(Me)2,Arg6,Tyr-NH29]AVP Peptide Click here for species-specific activity table Hs Antagonist 6.5 pKi 83
⤷ pKi 6.5 [83]
OH-LVA Peptide Click here for species-specific activity table Hs Antagonist 6.4 pKi 83
⤷ pKi 6.4 [83]
YM 218 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 6.4 pKi 80
⤷ pKi 6.4 [80]
d(CH2)5[Tyr(Me)2,Thr4,Tyr-NH29]OVT Peptide Click here for species-specific activity table Hs Antagonist 6.0 pKi 74,83
⤷ pKi 6.0 [74,83]
nelivaptan Small molecule or natural product Click here for species-specific activity table Hs Antagonist 5.9 pKi 76
⤷ pKi 5.9 [76]
atosiban Peptide Approved drug Click here for species-specific activity table Hs Antagonist 5.5 – 6.0 pKi 15,75
⤷ pKi 5.5 – 6.0 [15,75]
[Phaa1,D-Tyr(Et)2,Val4,Lys6,Tyr-NH28,des-Gly9]AVP Peptide Click here for species-specific activity table Hs Antagonist 5.7 pKi 83
⤷ pKi 5.7 [83]
d(CH2)5[Tyr(Me)2,Thr4]OVT Peptide Click here for species-specific activity table Hs Antagonist 5.2 pKi 83
⤷ pKi 5.2 [83]
Ro5028442 Small molecule or natural product Click here for species-specific activity table Hs Antagonist <4.5 pKi 62
⤷ pKi <4.5 (Ki >3x10-5 M) [62]
OPC-21268 Small molecule or natural product Click here for species-specific activity table Hs Antagonist 4.5 pKi 83
⤷ pKi 4.5 [83]
View species-specific antagonist tables
Immuno Process Associations
Immuno Process:  Cellular signalling
Immuno Process:  Cytokine production & signalling
Primary Transduction Mechanisms Click here for help
Transducer Effector/Response
Gs family Adenylyl cyclase stimulation
References:  70
Tissue Distribution Click here for help
Lung.
Species:  Human
Technique:  RT-PCR and Northern Blotting.
References:  25
Adult: cerebellum (no change during development).
Newborn: cerebellum, choroid plexus, hippocampus.
Species:  Human
Technique:  RT-PCR and Immunohistochemistry.
References:  39
Kidney: collecting duct, distal convoluted tubule/connecting tubule.
Species:  Rat
Technique:  Immunohistochemistry.
References:  27
Hippocampus.
Species:  Rat
Technique:  RT-PCR.
References:  36
Adult: kidney.
Newborn: brain, kidney.
Species:  Rat
Technique:  RT-PCR.
References:  35
Kidney.
Species:  Rat
Technique:  in situ hybridisation.
References:  57
Kidney: cortical collecting duct, outer medullary collecting duct, inner medullary collecting duct > inner medullary thick limbs, medullary thick ascending limbs, initial cortical collecting duct.
Species:  Rat
Technique:  RT-PCR.
References:  82
Kidney: medullary thick ascending limb, cortical thick ascending limb, cortical collecting duct, outer medullary collecting duct, inner medullary collecting duct.
Species:  Rat
Technique:  Immunohistochemistry.
References:  52
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 cAMP levels in CHO cells transfected with the human V2 receptor.
Species:  Human
Tissue:  CHO cells.
Response measured:  Stimulation of cAMP accumulation.
References:  79
Measurement of cAMP-sensitive reporter gene activity levels in L cells transfected with the rat V2 receptor.
Species:  Rat
Tissue:  L cells.
Response measured:  Stimulation of acitivity of cAMP-sensitive reporter gene.
References:  45
Measurement of cAMP levels in cultured hippocampal neurons endogenously expressing the putative rat V2 receptor.
Species:  Rat
Tissue:  Cultured hippocampal neurons.
Response measured:  Stimulation of cAMP accumulation.
References:  22
Measurement of cAMP levels in a tubular suspension of medullary thick ascending limb of Henle's loop endogenously expressing the V2 receptor.
Species:  Rat
Tissue:  Medullary thick ascending limb of Henle's loop.
Response measured:  Stimulation of cAMP accumulation.
References:  41
Physiological Functions Click here for help
Water homeostasis (antidiuretic).
Species:  Rat
Tissue:  In vivo (kidney).
References:  40,49
Nitric oxide production (via the phosphoinositide pathway).
Species:  Rat
Tissue:  Inner medullary collecting duct.
References:  53
Stimulation of an increase in osmotic water permeability.
Species:  Rat
Tissue:  Inner medullary collecting duct.
References:  14
Potentiation of pilocarpine-induced seizures.
Species:  Rat
Tissue:  In vivo (brain).
References:  18
Modulation of nociception.
Species:  Rat
Tissue:  Periaqueductal gray.
References:  90
Regulation of aquaporin-2 (AQP2) expression.
Species:  Rat
Tissue:  In vivo (kidney).
References:  61
Stimulation of renal medullary blood flow.
Species:  Rat
Tissue:  In vivo (kidney).
References:  51
Physiological Consequences of Altering Gene Expression Click here for help
Mice with siRNA-mediated inhibition of V2 receptor expression in the kidney exhibit a reduced antidiuretic action in response to vasopressin.
Species:  Mouse
Tissue: 
Technique:  RNA interference.
References:  34
Rats with siRNA-mediated inhibition of V2 receptor expression in the periaqueductal gray exhibit a decreased pain threshold.
Species:  Rat
Tissue: 
Technique:  RNA interference.
References:  90
Gene transfer of human AVPR2 into rat myocardium in vivo results in a positive inotropic effect.
Species:  Human
Tissue: 
Technique:  Adenoviral gene transfer.
References:  87
Gene transfer of human AVPR2 into rat cardiomyocyes results in potentiation of contractile force.
Species:  Human
Tissue: 
Technique:  Adenoviral gene transfer.
References:  44
Induction of a nonsense mutation into the AVPR2 receptor gene (Glu198 -> STOP) results in an X-linked nephrogenic diabetes insipidus-like phenotype.
Species:  Mouse
Tissue: 
Technique:  Induced mutation.
References:  91
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
Avpr2+|Avpr2tm1Jwe Avpr2tm1Jwe/Avpr2+
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0002136 abnormal kidney physiology PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0001262 decreased body weight PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0002988 decreased urine osmolality PMID: 11104789 
Avpr2+|Avpr2tm1Jwe Avpr2tm1Jwe/Avpr2+
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0002988 decreased urine osmolality PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0003853 dry skin PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0000519 hydronephrosis PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0000189 hypoglycemia PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0003019 increased circulating chloride level PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0005633 increased circulating sodium level PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0002608 increased hematocrit PMID: 11104789 
Avpr2+|Avpr2tm1Jwe Avpr2tm1Jwe/Avpr2+
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0001426 polydipsia PMID: 11104789 
Avpr2+|Avpr2tm1Jwe Avpr2tm1Jwe/Avpr2+
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0001762 polyuria PMID: 11104789 
Avpr2tm1Jwe Avpr2tm1Jwe/Y
involves: 129S1/Sv * 129X1/SvJ * CF-1		 MGI:88123  MP:0002082 postnatal lethality PMID: 11104789 
Clinically-Relevant Mutations and Pathophysiology Click here for help
Disease:  Nephrogenic diabetes insipidus
Disease Ontology: DOID:12387
OMIM: 304800
Orphanet: ORPHA223
Comments:  183 mutations of the AVPR2 gene have been found in X-linked nephrogenic diabetes insipidus patients. 89 missense, 18 nonsense, 45 frameshift deletion or insertion, 7 in-frame deletion or insertion, 4 splice-site, 19 large deletion, 1 complex mutation.
References:  2-3,5-7,10,12,20,23,31,37-38,42-43,45,47-48,55-56,58-59,63-64,67,71-72,77,81,85-86,88
Disease:  Nephrogenic syndrome of inappropriate antidiuresis
Synonyms: Inappropriate antidiuretic hormone secretion syndrome [Orphanet: ORPHA83449]
OMIM: 300539
Orphanet: ORPHA83449
Comments:  Activating mutations have been identified in the AVPR2 gene resulting in a syndrome termed "nephrogenic syndrome of inappropriate antidiuresis" (NSIAD), a common cause of familial hyponatremia.
References:  26,32,65
Biologically Significant Variants Click here for help
Type:  Splice variants
Species:  Rat
Description:  Two splice variants of the V2 receptor have been found in the rat kidney tubules. The longer most abundent form, V2(L), and the shorter form, V2(S), which lacks the 7th transmembrane domain and does not couple to the AC pathway.
References:  28
General Comments
One of the main endocrine functions of arginine vasopressin (AVP, also called ADH) is the facilitation of water re-absorption by the kidney through its action on the V2 vasopressin receptor. Vasopressin inhibits diuresis by binding to V2 vasopressin receptors present on the basolateral membrane of the renal collecting duct cells. The activation of the V2 receptor in renal collecting tubules stimulates adenylate cyclase type 6 through Gs and promotes the cyclic adenosine monophosphate- and protein kinase A-mediated incorporation of water channels (aquaporin 2) into the luminal surface of these cells. Long-term V2 receptor occupation also increases the total aquaporin-2 in the cell through a transcriptional mechanism. The AVP analog dDAVP (desmopressin) is a selective V2 agonist used for the treatment of central diabetes insipidus. It is also used to treat bleeding episodes in patients suffering from hemophilia A and Von Willebrand?s disease, the most frequent congenital bleeding disorders. The possible existence of other extra-renal V2 receptors in mammals is still an open question.

Some molecular biological studies suggesting the presence of extra-renal V2 receptors should be interpreted with caution since the ARHGAP4 (a member of the RhoGTPase activating protein family) gene is immediately adjacent to and orientated towards the V2 receptor gene on opposite strands - the transcriptional units of each gene overlap [29]. Molecular probes (e.g., cDNAs) or primers (e.g., for PCR) to detect V2 receptor mRNA must be carefully designed to exclude detection of ARHGAP4 mRNA. ARHGAP4 is present in specific brain regions including hippocampus, brainstem, striatum and cerebellum [29].

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]

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