S1P2 receptor

Target id: 276

Nomenclature: S1P2 receptor

Family: Lysophospholipid (S1P) receptors

Annotation status:  image of a green circle Annotated and expert reviewed. Please contact us if you can help with updates.  » Email us

   GtoImmuPdb view: OFF :     S1P2 receptor has curated GtoImmuPdb data

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 353 19p13.2 S1PR2 sphingosine-1-phosphate receptor 2
Mouse 7 352 9 A3 S1pr2 sphingosine-1-phosphate receptor 2
Rat 7 352 8q13 S1pr2 sphingosine-1-phosphate receptor 2
Previous and Unofficial Names
edg5 | Gpcr13 | endothelial differentiation G protein-coupled receptor 5 | G protein-coupled receptor 13 | GPCR18 | S1P receptor 2
Database Links
Specialist databases
GPCRDB s1pr2_human (Hs), s1pr2_mouse (Mm), s1pr2_rat (Rn)
Other databases
ChEMBL Target
Ensembl Gene
Entrez Gene
GenitoUrinary Development Molecular Anatomy Project
Human Protein Atlas
KEGG Gene
OMIM
RefSeq Nucleotide
RefSeq Protein
UniProtKB
Wikipedia
Natural/Endogenous Ligands
sphingosine 1-phosphate
sphingosylphosphorylcholine
Comments: Sphingosine 1-phosphate exhibits greater potency than sphingosylphosphorylcholine
Potency order of endogenous ligands
sphingosine 1-phosphate > dihydrosphingosine 1-phosphate > sphingosylphosphorylcholine  [2,25]

Download all structure-activity data for this target as a CSV file

Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
sphingosine 1-phosphate Hs Agonist 7.6 – 7.7 pKd 15,36
pKd 7.6 – 7.7 (Kd 2.7x10-8 – 2.04x10-8 M) [15,36]
sphingosine 1-phosphate Mm Agonist 8.7 pEC50 31
pEC50 8.7 (EC50 2x10-9 M) [31]
sphingosine 1-phosphate Hs Agonist 8.1 – 8.5 pEC50 10,29
pEC50 8.1 – 8.5 [10,29]
FTY720-phosphate Hs Agonist 7.5 pEC50 34
pEC50 7.5 (EC50 3.5x10-8 M) Measured using an impedance-based assay system [34]
ozanimod Hs Agonist <5.0 pEC50 32
pEC50 <5.0 (EC50 >1x10-5 M) [32]
Description: In a GTPγS assay.
AUY954 Mm Agonist 4.7 – 5.0 pEC50 29
pEC50 4.7 – 5.0 [29]
compound 43 [PMID: 26751273] Hs Agonist >4.5 pEC50 5
pEC50 >4.5 (EC50 <3.163x10-5 M) [5]
Description: In a S1P2R yeast reporter assay.
View species-specific agonist tables
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
compound 16 [PMID: 26794040] Hs Antagonist 8.1 pIC50 19
pIC50 8.1 (IC50 8.2x10-9 M) [19]
JTE-013 Hs Antagonist 7.8 pIC50 27
pIC50 7.8 (IC50 1.7x10-8 M) [27]
JTE-013 Rn Antagonist 7.7 – 7.8 pIC50 9,27
pIC50 7.7 – 7.8 (IC50 2.2x10-8 – 1.7x10-8 M) [9,27]
View species-specific antagonist tables
Immunopharmacology Comments
Activation of S1P2R has pro-inflammatory effects (e.g. mast cell degranulation, regulation of pro-inflammatory cytokine production, and cytokine and chemokine release [18,28]. In human cord blood mast cells, S1P2R positively regulates allergen-induced degranulation and chemokine release [26,30].
Immuno Cell Type Associations
Immuno Cell Type:  Mast cells
Cell Ontology Term:   mast cell (CL:0000097)
Comment:  Cord blood mast cells express S1P1R and S1P2R
References:  20
Primary Transduction Mechanisms
Transducer Effector/Response
Gs family
Gq/G11 family
G12/G13 family
Adenylate cyclase stimulation
Phospholipase C stimulation
Calcium channel
Comments:  Activation of Rho, MAPK, and phosphorylation of MLC [6].
References:  6,13
Tissue Distribution
Adult heart, lung
Expression level:  High
Species:  Mouse
Technique:  Northern blot analysis
References:  37
Embryonic brain
Expression level:  High
Species:  Mouse
Technique:  RT-PCR, Northern hybridization analysis
References:  22-23,38
Heart, lung, kidney, liver, and thymus
Species:  Mouse
Technique:  Northern blot
References:  38
Expression Datasets

Show »

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]

There should be a chart of expression data here, you may need to enable JavaScript!
Functional Assays
Cell proliferation and survival
Species:  Human
Tissue:  HTC4 hepatoma cells stably transfected with human S1P2
Response measured: 
References:  1
Negative regulation of cell motility
Species:  Mouse
Tissue:  B16 melanoma cell
Response measured: 
References:  3
Negative regulation of endothelial morphogenesis and angiogenesis
Species:  Mouse
Tissue:  Vascular endothelial cells
Response measured: 
References:  11
Physiological Consequences of Altering Gene Expression
Severe vascular phenotype in S1P2/S1P3 double and S1P1/S1P2/S1P3 triple knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  17
Eyelid closure during embryonic development in S1P2/S1P3 double knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  8
Loss of phagocytic activity in receptor knockout macrophages
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  24
Suppression of vasoconstriction in knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  35
Development of clonal B-cell lymphomas with age in knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  4
Suppression of pathologic neovascularization in knockout mice
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  33
Deafness and stria vascularis defects
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  7,16,21
No gross anatomical abnormalities, but spontaneous seizures (3 – 7 weeks of age) and neuronal hyperexcitability
Species:  Mouse
Tissue: 
Technique:  Gene targeting (replacement vector with LacZ marker gene, deletion of entire ORF)
References:  23
Slightly reduced viability; normal development and fertility
Species:  Mouse
Tissue: 
Technique:  Gene knockout
References:  12
Phenotypes, Alleles and Disease Models Mouse data from MGI

Show »

Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
involves: 129S5/SvEvBrd * C57BL/6
MGI:99569  MP:0005402 abnormal action potential PMID: 11553273 
S1pr1tm1Rlp|S1pr2tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:99569  MP:0000260 abnormal angiogenesis PMID: 15138255 
S1pr1tm1Rlp|S1pr2tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MGI:99569  MP:0000260 abnormal angiogenesis PMID: 15138255 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
involves: 129S5/SvEvBrd * C57BL/6
MGI:99569  MP:0004994 abnormal brain wave pattern PMID: 11553273 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
involves: 129S5/SvEvBrd * C57BL/6
MGI:99569  MP:0002206 abnormal CNS synaptic transmission PMID: 11553273 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
involves: 129S5/SvEvBrd * C57BL/6
MGI:99569  MP:0002910 abnormal excitatory postsynaptic currents PMID: 11553273 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0001386 abnormal maternal nurturing PMID: 12006579 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
involves: 129S5/SvEvBrd * C57BL/6
MGI:99569  MP:0002272 abnormal nervous system electrophysiology PMID: 11553273 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0001504 abnormal posture PMID: 17287522 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0004305 abnormal Rosenthal canal morphology PMID: 16945494 
S1pr2tm1Rlp|S1pr3tm1Rlp S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1339365  MGI:99569  MP:0004244 abnormal spontaneous abortion rate PMID: 15138255 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0004365 abnormal strial basal cells PMID: 17284444 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0004367 abnormal strial intermediate cells PMID: 17284444 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0004366 abnormal strial marginal cells PMID: 17284444 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0000048 abnormal stria vascularis PMID: 17284444 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0004368 abnormal stria vascularis vasculature morphology PMID: 17284444 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0003149 abnormal tectorial membrane morphology PMID: 16945494 
S1pr2tm1Rlp|S1pr3tm1Rlp S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1339365  MGI:99569  MP:0006055 abnormal vascular endothelial cell morphology PMID: 15138255 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0004427 abnormal vestibular labyrinth PMID: 17284444 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0004742 abnormal vestibular system physiology PMID: 17287522 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0004742 abnormal vestibular system physiology PMID: 16945494 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0000034 abnormal vestibule morphology PMID: 17287522 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0004763 absent brainstem auditory evoked potential PMID: 17284444 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0004763 absent brainstem auditory evoked potential PMID: 16945494 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0004737 absent distortion product otoacoustic emissions PMID: 17284444 
S1pr2tm1Jch S1pr2tm1Jch/S1pr2tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:99569  MP:0006359 absent startle reflex PMID: 17287522 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0006359 absent startle reflex PMID: 17287522 
S1pr2tm1Jch|S1pr3+|S1pr3tm1Jch S1pr3tm1Jch/S1pr3+,S1pr2tm1Jch/S1pr2tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0006359 absent startle reflex PMID: 17287522 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0004518 absent vestibular hair cell stereocilia PMID: 17287522 
S1pr2tm1Rlp|S1pr3tm1Rlp S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1339365  MGI:99569  MP:0002857 cochlear ganglion degeneration PMID: 17284444 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0002857 cochlear ganglion degeneration PMID: 17284444 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0002857 cochlear ganglion degeneration PMID: 17287522 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0004362 cochlear hair cell degeneration PMID: 17284444 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0004398 cochlear inner hair cell degeneration PMID: 17287522 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0004404 cochlear outer hair cell degeneration PMID: 17287522 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0004404 cochlear outer hair cell degeneration PMID: 16945494 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0001967 deafness PMID: 17284444 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0001967 deafness PMID: 16945494 
S1pr2tm1Jch S1pr2tm1Jch/S1pr2tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:99569  MP:0001935 decreased litter size PMID: 12006579 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0001935 decreased litter size PMID: 12006579 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0003144 decreased otolith number PMID: 17284444 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0003144 decreased otolith number PMID: 16945494 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0002757 decreased vertical activity PMID: 17287522 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0004465 degeneration of organ of Corti supporting cells PMID: 17287522 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0006023 detached Reissner membrane PMID: 16945494 
S1pr1tm1Rlp|S1pr2tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:99569  MP:0006207 embryonic lethality during organogenesis PMID: 15138255 
S1pr1tm1Rlp|S1pr2tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MGI:99569  MP:0006207 embryonic lethality during organogenesis PMID: 15138255 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0003143 enlarged otoliths PMID: 17284444 
S1pr2tm1Rlp|S1pr3tm1Rlp S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1339365  MGI:99569  MP:0005191 head tilt PMID: 17284444 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0005191 head tilt PMID: 17284444 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0005191 head tilt PMID: 17287522 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0005191 head tilt PMID: 16945494 
S1pr2tm1Rlp|S1pr3tm1Rlp S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1339365  MGI:99569  MP:0001914 hemorrhage PMID: 15138255 
S1pr1tm1Rlp|S1pr2tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:99569  MP:0001914 hemorrhage PMID: 15138255 
S1pr1tm1Rlp|S1pr2tm1Rlp|S1pr3tm1Rlp S1pr1tm1Rlp/S1pr1tm1Rlp,S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1096355  MGI:1339365  MGI:99569  MP:0001914 hemorrhage PMID: 15138255 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0001523 impaired righting response PMID: 17287522 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0001522 impaired swimming PMID: 17287522 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0001522 impaired swimming PMID: 16945494 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0001513 limb grasping PMID: 17287522 
S1pr2tm1Rlp S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:99569  MP:0000043 organ of Corti degeneration PMID: 17284444 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0000043 organ of Corti degeneration PMID: 17287522 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0000043 organ of Corti degeneration PMID: 16945494 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0004897 otosclerosis PMID: 16945494 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0002081 perinatal lethality PMID: 12006579 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0002083 premature death PMID: 16945494 
S1pr2tm1Rlp|S1pr3tm1Rlp S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1339365  MGI:99569  MP:0002080 prenatal lethality PMID: 15138255  17284444 
S1pr2tm1Rlp|S1pr3tm1Rlp S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1339365  MGI:99569  MP:0001921 reduced fertility PMID: 15138255 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0004329 saccular degeneration PMID: 16945494 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0004331 saccular macula degeneration PMID: 17287522 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
involves: 129S5/SvEvBrd * C57BL/6
MGI:99569  MP:0002064 seizures PMID: 11553273 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0002064 seizures PMID: 16945494 
S1pr2tm1Rlp|S1pr3tm1Rlp S1pr3tm1Rlp/S1pr3tm1Rlp,S1pr2tm1Rlp/S1pr2tm1Rlp
involves: 129S6/SvEvTac * C57BL/6
MGI:1339365  MGI:99569  MP:0001786 skin edema PMID: 15138255 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0008308 small scala media PMID: 16945494 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
either: (involves: 129S5/SvEvBrd) or (involves: 129S5/SvEvBrd * C57BL/6)
MGI:99569  MP:0004364 thin stria vascularis PMID: 16945494 
S1pr2tm1Ajml S1pr2tm1Ajml/S1pr2tm1Ajml
involves: 129S5/SvEvBrd * C57BL/6
MGI:99569  MP:0003997 tonic-clonic seizures PMID: 11553273 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0004334 utricular macular degeneration PMID: 17287522 
S1pr2tm1Jch|S1pr3tm1Jch S1pr2tm1Jch/S1pr2tm1Jch,S1pr3tm1Jch/S1pr3tm1Jch
involves: 129S1/Sv * 129X1/SvJ * C57BL/6N
MGI:1339365  MGI:99569  MP:0004324 vestibular hair cell degeneration PMID: 17287522 
General Comments
S1P2 receptor has been shown to be a specific receptor for the central nervous system membrane protein Nogo-A-Δ20 [14].

References

Show »

1. An S, Zheng Y, Bleu T. (2000) Sphingosine 1-phosphate-induced cell proliferation, survival, and related signaling events mediated by G protein-coupled receptors Edg3 and Edg5. J. Biol. Chem.275 (1): 288-96. [PMID:10617617]

2. Ancellin N, Hla T. (1999) Differential pharmacological properties and signal transduction of the sphingosine 1-phosphate receptors EDG-1, EDG-3, and EDG-5. J. Biol. Chem.274 (27): 18997-9002. [PMID:10383399]

3. Arikawa K, Takuwa N, Yamaguchi H, Sugimoto N, Kitayama J, Nagawa H, Takehara K, Takuwa Y. (2003) Ligand-dependent inhibition of B16 melanoma cell migration and invasion via endogenous S1P2 G protein-coupled receptor. Requirement of inhibition of cellular RAC activity. J. Biol. Chem.278 (35): 32841-51. [PMID:12810709]

4. Cattoretti G, Mandelbaum J, Lee N, Chaves AH, Mahler AM, Chadburn A, Dalla-Favera R, Pasqualucci L, MacLennan AJ. (2009) Targeted disruption of the S1P2 sphingosine 1-phosphate receptor gene leads to diffuse large B-cell lymphoma formation. Cancer Res.69 (22): 8686-92. [PMID:19903857]

5. Demont EH, Bailey JM, Bit RA, Brown JA, Campbell CA, Deeks N, Dowell SJ, Eldred C, Gaskin P, Gray JR et al.. (2016) Discovery of Tetrahydropyrazolopyridine as Sphingosine 1-Phosphate Receptor 3 (S1P3)-Sparing S1P1 Agonists Active at Low Oral Doses. J. Med. Chem.59 (3): 1003-20. [PMID:26751273]

6. Gonda K, Okamoto H, Takuwa N, Yatomi Y, Okazaki H, Sakurai T, Kimura S, Sillard R, Harii K, Takuwa Y. (1999) The novel sphingosine 1-phosphate receptor AGR16 is coupled via pertussis toxin-sensitive and -insensitive G-proteins to multiple signalling pathways. Biochem. J.337 ( Pt 1): 67-75. [PMID:9854026]

7. Herr DR, Grillet N, Schwander M, Rivera R, Müller U, Chun J. (2007) Sphingosine 1-phosphate (S1P) signaling is required for maintenance of hair cells mainly via activation of S1P2. J. Neurosci.27 (6): 1474-8. [PMID:17287522]

8. Herr DR, Lee CW, Wang W, Ware A, Rivera R, Chun J. (2013) Sphingosine 1-phosphate receptors are essential mediators of eyelid closure during embryonic development. J. Biol. Chem.288 (41): 29882-9. [PMID:24003216]

9. Ikeda H, Satoh H, Yanase M, Inoue Y, Tomiya T, Arai M, Tejima K, Nagashima K, Maekawa H, Yahagi N et al.. (2003) Antiproliferative property of sphingosine 1-phosphate in rat hepatocytes involves activation of Rho via Edg-5. Gastroenterology124 (2): 459-69. [PMID:12557151]

10. Im DS, Clemens J, Macdonald TL, Lynch KR. (2001) Characterization of the human and mouse sphingosine 1-phosphate receptor, S1P5 (Edg-8): structure-activity relationship of sphingosine1-phosphate receptors. Biochemistry40 (46): 14053-60. [PMID:11705398]

11. Inoki I, Takuwa N, Sugimoto N, Yoshioka K, Takata S, Kaneko S, Takuwa Y. (2006) Negative regulation of endothelial morphogenesis and angiogenesis by S1P2 receptor. Biochem. Biophys. Res. Commun.346 (1): 293-300. [PMID:16756949]

12. Ishii I, Ye X, Friedman B, Kawamura S, Contos JJ, Kingsbury MA, Yang AH, Zhang G, Brown JH, Chun J. (2002) Marked perinatal lethality and cellular signaling deficits in mice null for the two sphingosine 1-phosphate (S1P) receptors, S1P(2)/LP(B2)/EDG-5 and S1P(3)/LP(B3)/EDG-3. J. Biol. Chem.277 (28): 25152-9. [PMID:12006579]

13. Jiang LI, Collins J, Davis R, Lin KM, DeCamp D, Roach T, Hsueh R, Rebres RA, Ross EM, Taussig R et al.. (2007) Use of a cAMP BRET sensor to characterize a novel regulation of cAMP by the sphingosine 1-phosphate/G13 pathway. J. Biol. Chem.282 (14): 10576-84. [PMID:17283075]

14. Kempf A, Tews B, Arzt ME, Weinmann O, Obermair FJ, Pernet V, Zagrebelsky M, Delekate A, Iobbi C, Zemmar A et al.. (2014) The Sphingolipid Receptor S1PR2 Is a Receptor for Nogo-A Repressing Synaptic Plasticity. PLoS Biol.12 (1): e1001763. [PMID:24453941]

15. Kon J, Sato K, Watanabe T, Tomura H, Kuwabara A, Kimura T, Tamama K, Ishizuka T, Murata N, Kanda T et al.. (1999) Comparison of intrinsic activities of the putative sphingosine 1-phosphate receptor subtypes to regulate several signaling pathways in their cDNA-transfected Chinese hamster ovary cells. J. Biol. Chem.274 (34): 23940-7. [PMID:10446161]

16. Kono M, Belyantseva IA, Skoura A, Frolenkov GI, Starost MF, Dreier JL, Lidington D, Bolz SS, Friedman TB, Hla T et al.. (2007) Deafness and stria vascularis defects in S1P2 receptor-null mice. J. Biol. Chem.282 (14): 10690-6. [PMID:17284444]

17. Kono M, Mi Y, Liu Y, Sasaki T, Allende ML, Wu YP, Yamashita T, Proia RL. (2004) The sphingosine-1-phosphate receptors S1P1, S1P2, and S1P3 function coordinately during embryonic angiogenesis. J. Biol. Chem.279 (28): 29367-73. [PMID:15138255]

18. Kulinski JM, Muñoz-Cano R, Olivera A. (2016) Sphingosine-1-phosphate and other lipid mediators generated by mast cells as critical players in allergy and mast cell function. Eur. J. Pharmacol.778: 56-67. [PMID:25941085]

19. Kusumi K, Shinozaki K, Yamaura Y, Hashimoto A, Kurata H, Naganawa A, Otsuki K, Matsushita T, Sekiguchi T, Kakuuchi A et al.. (2016) Discovery of novel S1P2 antagonists, part 3: Improving the oral bioavailability of a series of 1,3-bis(aryloxy)benzene derivatives. Bioorg. Med. Chem. Lett.26 (4): 1209-13. [PMID:26794040]

20. Mackle T, Gendy SS, Walsh M, McConn-Walsh R, Costello RW, Walsh MT. (2008) Role of sphingosine 1-phosphate receptor expression in eosinophils of patients with allergic rhinitis, and effect of topical nasal steroid treatment on this receptor expression. J Laryngol Otol122 (12): 1309-17. [PMID:18808729]

21. MacLennan AJ, Benner SJ, Andringa A, Chaves AH, Rosing JL, Vesey R, Karpman AM, Cronier SA, Lee N, Erway LC et al.. (2006) The S1P2 sphingosine 1-phosphate receptor is essential for auditory and vestibular function. Hear. Res.220 (1-2): 38-48. [PMID:16945494]

22. MacLennan AJ, Browe CS, Gaskin AA, Lado DC, Shaw G. (1994) Cloning and characterization of a putative G-protein coupled receptor potentially involved in development. Mol. Cell. Neurosci.5 (3): 201-9. [PMID:8087418]

23. MacLennan AJ, Carney PR, Zhu WJ, Chaves AH, Garcia J, Grimes JR, Anderson KJ, Roper SN, Lee N. (2001) An essential role for the H218/AGR16/Edg-5/LP(B2) sphingosine 1-phosphate receptor in neuronal excitability. Eur. J. Neurosci.14 (2): 203-9. [PMID:11553273]

24. McQuiston T, Luberto C, Del Poeta M. (2011) Role of sphingosine-1-phosphate (S1P) and S1P receptor 2 in the phagocytosis of Cryptococcus neoformans by alveolar macrophages. Microbiology (Reading, Engl.)157 (Pt 5): 1416-27. [PMID:21292747]

25. Okamoto H, Takuwa N, Gonda K, Okazaki H, Chang K, Yatomi Y, Shigematsu H, Takuwa Y. (1998) EDG1 is a functional sphingosine-1-phosphate receptor that is linked via a Gi/o to multiple signaling pathways, including phospholipase C activation, Ca2+ mobilization, Ras-mitogen-activated protein kinase activation, and adenylate cyclase inhibition. J. Biol. Chem.273 (42): 27104-10. [PMID:9765227]

26. Olivera A. (2008) Unraveling the complexities of sphingosine-1-phosphate function: the mast cell model. Prostaglandins Other Lipid Mediat.86 (1-4): 1-11. [PMID:18403224]

27. Osada M, Yatomi Y, Ohmori T, Ikeda H, Ozaki Y. (2002) Enhancement of sphingosine 1-phosphate-induced migration of vascular endothelial cells and smooth muscle cells by an EDG-5 antagonist. Biochem. Biophys. Res. Commun.299 (3): 483-7. [PMID:12445827]

28. Oskeritzian CA, Price MM, Hait NC, Kapitonov D, Falanga YT, Morales JK, Ryan JJ, Milstien S, Spiegel S. (2010) Essential roles of sphingosine-1-phosphate receptor 2 in human mast cell activation, anaphylaxis, and pulmonary edema. J. Exp. Med.207 (3): 465-74. [PMID:20194630]

29. Pan S, Mi Y, Pally C, Beerli C, Chen A, Guerini D, Hinterding K, Nuesslein-Hildesheim B, Tuntland T, Lefebvre S et al.. (2006) A monoselective sphingosine-1-phosphate receptor-1 agonist prevents allograft rejection in a stringent rat heart transplantation model. Chem. Biol.13 (11): 1227-34. [PMID:17114004]

30. Price MM, Oskeritzian CA, Milstien S, Spiegel S. (2008) Sphingosine-1-phosphate synthesis and functions in mast cells. Future Lipidol3 (6): 665-674. [PMID:19802381]

31. Sanna MG, Liao J, Jo E, Alfonso C, Ahn MY, Peterson MS, Webb B, Lefebvre S, Chun J, Gray N et al.. (2004) Sphingosine 1-phosphate (S1P) receptor subtypes S1P1 and S1P3, respectively, regulate lymphocyte recirculation and heart rate. J. Biol. Chem.279 (14): 13839-48. [PMID:14732717]

32. Scott FL, Clemons B, Brooks J, Brahmachary E, Powell R, Dedman H, Desale HG, Timony GA, Martinborough E, Rosen H et al.. (2016) Ozanimod (RPC1063) is a potent sphingosine-1-phosphate receptor-1 (S1P1 ) and receptor-5 (S1P5 ) agonist with autoimmune disease-modifying activity. Br. J. Pharmacol.173 (11): 1778-92. [PMID:26990079]

33. Skoura A, Sanchez T, Claffey K, Mandala SM, Proia RL, Hla T. (2007) Essential role of sphingosine 1-phosphate receptor 2 in pathological angiogenesis of the mouse retina. J. Clin. Invest.117 (9): 2506-16. [PMID:17710232]

34. Sobel K, Monnier L, Menyhart K, Bolinger M, Studer R, Nayler O, Gatfield J. (2015) FTY720 Phosphate Activates Sphingosine-1-Phosphate Receptor 2 and Selectively Couples to Gα12/13/Rho/ROCK to Induce Myofibroblast Contraction. Mol. Pharmacol.87 (6): 916-27. [PMID:25762025]

35. Szczepaniak WS, Pitt BR, McVerry BJ. (2010) S1P2 receptor-dependent Rho-kinase activation mediates vasoconstriction in the murine pulmonary circulation induced by sphingosine 1-phosphate. Am. J. Physiol. Lung Cell Mol. Physiol.299 (1): L137-45. [PMID:20435688]

36. Van Brocklyn JR, Tu Z, Edsall LC, Schmidt RR, Spiegel S. (1999) Sphingosine 1-phosphate-induced cell rounding and neurite retraction are mediated by the G protein-coupled receptor H218. J. Biol. Chem.274 (8): 4626-32. [PMID:9988698]

37. Yang AH, Ishii I, Chun J. (2002) In vivo roles of lysophospholipid receptors revealed by gene targeting studies in mice. Biochim. Biophys. Acta1582 (1-3): 197-203. [PMID:12069829]

38. Zhang G, Contos JJ, Weiner JA, Fukushima N, Chun J. (1999) Comparative analysis of three murine G-protein coupled receptors activated by sphingosine-1-phosphate. Gene227 (1): 89-99. [PMID:9931453]

Contributors

Show »

How to cite this page

Yasuyuki Kihara, Victoria Blaho, Hirotaka Mizuno, Jerold Chun.
Lysophospholipid (S1P) receptors: S1P2 receptor. Last modified on 10/03/2017. Accessed on 21/10/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/ObjectDisplayForward?objectId=276.