Nomenclature: P2Y1 receptor

Family: P2Y receptors

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Contents

Gene and Protein Information
class A G protein-coupled receptor
Species TM AA Chromosomal Location Gene Symbol Gene Name Reference
Human 7 373 3q25.2 P2RY1 purinergic receptor P2Y, G-protein coupled, 1 1,26
Mouse 7 373 3 E1 P2ry1 purinergic receptor P2Y, G-protein coupled 1 49
Rat 7 373 2q31 P2ry1 purinergic receptor P2Y, G-protein coupled, 1 49
Previous and Unofficial Names
P2Y
Purinergic receptor P2Y1
ATP receptor
P2Y purinoceptor 1
platelet ADP receptor
P2 purinoceptor subtype Y1
purinergic receptor P2Y G-protein coupled 1
P2Y1
P2y
P2 purinoreceptor subclass 2Y
P2Y ATP receptor 1
purinergic receptor P2Y, G-protein coupled 1
purinergic receptor P2Y, G-protein coupled, 1
P2Y1 receptor
Database Links
ChEMBL Target
Ensembl Gene
Entrez Gene
GPCRDB
GeneCards
GenitoUrinary Development Molecular Anatomy Project
HomoloGene
Human Protein Reference Database
InterPro
KEGG Gene
OMIM
PharmGKB Gene
PhosphoSitePlus
Protein Ontology (PRO)
RefSeq Nucleotide
RefSeq Protein
TreeFam
UniGene Hs.
UniProtKB
Wikipedia
Natural/Endogenous Ligands
ADP
ATP
Rank order of potency
ADP>ATP
Agonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
MRS2365 Hs Agonist 9.4 pEC50 7
pEC50 9.4 [7]
compound 3a [PMID:22873688] Mg Full agonist 7.4 pEC50 51
pEC50 7.4 (EC50 3.8x10-8 M) [51]
ADPβS Hs Agonist 7.3 pEC50 47
pEC50 7.3 (EC50 4.99x10-8 M) [47]
2',3'-ddATP Hs Partial agonist 8.0 pIC50 42
pIC50 8.0 [42]
dATPαS Hs Partial agonist 7.7 pIC50 42
pIC50 7.7 [42]
ATPγS Hs Partial agonist 7.4 pIC50 42
pIC50 7.4 [42]
2MeSATP Hs Partial agonist 6.4 – 7.6 pIC50 42,50
pIC50 6.4 – 7.6 [42,50]
ATP Hs Partial agonist 6.1 – 7.8 pIC50 42,50
pIC50 6.1 – 7.8 [42,50]
ADP Hs Full agonist 6.2 – 7.2 pIC50 42,50
pIC50 6.2 – 7.2 [42,50]
2MeSADP Hs Full agonist 5.4 – 7.0 pIC50 42,50
pIC50 5.4 – 7.0 [42,50]
[3H]2MeSADP N/A Agonist - -
View species-specific agonist tables
Agonist Comments
ATP has been reported to be both a partial agonist [37] and an antagonist [22] (see Antagonist section).
Antagonists
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
[32P]MRS2500 Hs Antagonist 9.4 pKd 25
pKd 9.4 [25]
[3H]MRS2279 Hs Antagonist 8.1 pKd 50
pKd 8.1 (Kd 8x10-9 M) [50]
MRS2500 Hs Antagonist 8.8 – 9.1 pKi 5,28
pKi 8.8 – 9.1 [5,28]
BMS compound 16 [PMID:23368907] Hs Antagonist 8.2 pKi 6
pKi 8.2 (Ki 6x10-9 M) [6]
BMS compound 4c Hs Antagonist 8.2 pKi 40
pKi 8.2 (Ki 7x10-9 M) [40]
Pfizer compound 67 [PMID:18445527] Hs Antagonist 8.0 pKi 38
pKi 8.0 (Ki 1x10-8 M) [38]
MRS2279 Hs Antagonist 7.9 pKi 50
pKi 7.9 [50]
MRS2298 Hs Antagonist 7.5 pKi 5
pKi 7.5 [5]
Pfizer compound 11 [PMID:18445527] Hs Antagonist 7.3 pKi 38
pKi 7.3 (Ki 5x10-8 M) [38]
GlaxoSmithKline compound 6i [PMID:18926700] Hs Antagonist 7.2 pKi 36
pKi 7.2 (Ki 7x10-8 M) [36]
MRS2496 Hs Antagonist 7.1 pKi 5
pKi 7.1 [5]
MRS2179 Hs Antagonist 7.0 – 7.1 pKi 2,50
pKi 7.0 – 7.1 [2,50]
GlaxoSmithKline compound 5h [PMID:20542694] Hs Antagonist 6.85 pKi 48
pKi 6.85 (Ki 1.4x10-7 M) [48]
2,2'-pyridylisatogen tosylate Hs Antagonist 6.8 pKi 18
pKi 6.8 [18]
2-ClATP Hs Antagonist 5.6 pKi 22
pKi 5.6 [22]
suramin Hs Antagonist 5.3 pKi 50
pKi 5.3 [50]
PPADS Hs Antagonist 5.2 pKi 50
pKi 5.2 [50]
2MeSATP Hs Antagonist 5.2 pKi 22
pKi 5.2 [22]
ATP Hs Antagonist 4.8 pKi 22
pKi 4.8 [22]
A2P5P Hs Antagonist 5.8 pEC50 2
pEC50 5.8 [2]
adenosine-3'-5'-bisphosphate Hs Antagonist 5.6 pEC50 2
pEC50 5.6 [2]
MRS2950 Hs Antagonist 6.9 pIC50 8
pIC50 6.9 (IC50 1.4x10-7 M) [8]
Antagonist Comments
It is likely that ATP and derivatives (e.g. 2-ClATP and 2MeSATP) act as antagonists at P2Y1 rather than agonists. The apparent agonist action of these compounds may be due to impurity and to the rapid conversion to the diphosphate form [22]. High-throughput screening against the P2Y1 receptor identified a novel series of tetrahydro-4-quinolinamine antagonists [36].
Allosteric Modulators
Key to terms and symbols View all chemical structures Click column headers to sort
Ligand Sp. Action Affinity Units Reference
2,2'-pyridylisatogen tosylate Hs Negative 7.8 pIC50 17
pIC50 7.8 [17]
Primary Transduction Mechanisms
Transducer Effector/Response
Gq/G11 family Phospholipase C stimulation
Comments:  The activation of PLC leads to mobilisation of calcium from IP3-sensitive intracellular stores.
References:  10
Secondary Transduction Mechanisms
Transducer Effector/Response
Gi/Go family
Gq/G11 family
Potassium channel
Calcium channel
Comments:  In CHO cells stably expressing CFTR, the endogenous P2Y1 receptor shifts its coupling to Gi/Go [34]
References:  14,33
Tissue Distribution
Nucleus accumbens >> putamen > caudate nucleus, striatum > parahippocampal gyrus > hypothalamus, globus pallidus > cingulate gyrus, hippocampus > amygdala, medula oblongata > cerebellum, locus coeruleus, medial frontal gyrus, superior frontal gyrus, spinal cord > thalamus > substantia nigra.
Species:  Human
Technique:  RT-PCR.
References:  35
Placenta > prostate > brain > intestine > skeletal muscle, heart > macrophages > pituitary, lung > pancreas > spleen, foetal liver > adipose> stomach, lymphocytes > liver, kidney.
Species:  Human
Technique:  RT-PCR.
References:  35
Blood platelets.
Species:  Human
Technique:  RT-PCR
References:  27,31
GI tract: myenteric plexus, submucosal plexus, intestinal crypts of the ileum and along the lumen of the villi.
Species:  Mouse
Technique:  in situ hybridisation.
References:  19
Heart, skeletal muscle > brain, spleen, lung, liver, kidney.
Species:  Rat
Technique:  Northern blotting.
References:  49
Sensory ganglia: dorsal root ganglia (DRG), nodose ganglion (NG) and trigeminal ganglion (TG).
Species:  Rat
Technique:  RT-PCR and Immunohistochemistry.
References:  39
Expression Datasets

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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
Voltage clamp technique used to measure the ATP-evoked membrane current in Xenopus oocytes transfected with the P2Y1 receptor.
Species:  Rat
Tissue:  Xenopus oocytes.
Response measured:  Membrane current produced.
References:  49
Measurement of [Ca2+]i levels in Jurkat cells transfected with the P2Y1 receptor.
Species:  Human
Tissue:  Jurkat cells.
Response measured:  Increase in [Ca2+]i levels.
References:  21,31
Measurement of N-type Ca2+ channel currents in rat superior cervical ganglion (SCG) cells expressing the rat P2Y1 receptor.
Species:  Rat
Tissue:  Rat SCG cells.
Response measured:  Inhibition of N-type Ca2+ currents.
References:  13
Measurement of [Ca2+]i in human astrocytoma cells stably expressing the human P2Y1 receptor.
Species:  Human
Tissue:  1321N1 human astrocytoma cells.
Response measured:  Rapid increase in [Ca2+]i.
References:  37
Measurement of [Ca2+]i in rat glioma C6 cells endogenously expressing P2Y1 and P2Y2 receptors.
Species:  Rat
Tissue:  Glioma C6 cells.
Response measured:  Increase in [Ca2+]i via depletion of IP3-sensitive intracellular Ca2+ stores (PLC stimulation) and influx of extracellular Ca2+.
References:  41
Measurement of IP3 levels in response to selective P2Y1 receptor agonists in HEK 293 cells endogenously expressing the P2Y1 and P2Y2 receptors.
Species:  Human
Tissue:  HEK 293 cells.
Response measured:  Increase in IP3 accumulation.
References:  43
Measurement of Ca2+ levels in response to the P2Y1 agonist ADP in mouse peritoneal macrophages.
Species:  Mouse
Tissue:  Peritoneal macrophages.
Response measured:  Increase in [Ca2+]i.
References:  9
Measurement of K2+ current using patch-clamping of SCG cells transfected with the P2Y1 receptor and GIRK1 and GIRK2 channels.
Species:  Rat
Tissue:  SCG neurons.
Response measured:  Transient activation of GIRK current followed by inactivation.
References:  45
Following mechanical stimulation of an individual 1321N1 cell, measurement of Ca2+ propagation in 1321N1 cells transfected with the P2Y1 cells.
Species:  Rat
Tissue:  1321N1 cells.
Response measured:  Ca2+ wave only spread to cells expressing the P2Y1 receptor. P2Y1 is not required for the initiation of the wave.
References:  16
Measurement of K+ currents in primary cultures of pyramidal hippocampal neurons
Species:  Rat
Tissue:  Hippocampal primary neurons
Response measured:  Inhibition of the M-type K+ current
References:  14
Physiological Functions
Mitogenic effects.
Species:  Rat
Tissue:  Aortic smooth muscle cells.
References:  11
Smooth muscle relaxation.
Species:  Mouse
Tissue:  GI tract: stomach fundus, duodenum, ileum and colon.
References:  19
Vasodilation through the NO/cGMP pathway.
Species:  Rat
Tissue:  Arterial mesenteric bed.
References:  4
Platelet shape change.
Species:  Human
Tissue:  Platelets.
References:  27
Induction of platelet aggregation.
Species:  Human
Tissue:  Blood platelets.
References:  21
Release of IL-6 stimulation and enhanced neuroprotection
Species:  Rat
Tissue:  Primary hippocampal astrocytes
References:  15
GFAP and GDNF production under ischemic conditions
Species:  Rat
Tissue:  Astrocytes
References:  46
Atherosclerosis enhancement
Species:  Mouse
Tissue:  Aorta
References:  20
Glutamate efflux
Species:  Rat
Tissue:  Spinal cord astrocytes
References:  52
Endothelial cell migration
Species:  Human
Tissue:  HUVEC
References:  44
Regulation of EGF activity
Species:  Human
Tissue:  Epithelial cells
References:  3
Physiological Consequences of Altering Gene Expression
P2Y1 receptor knockout mice exhibit increased bleeding time and increased protection from collagen- and ADP-induced thromboembolism.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  12
P2Y1 receptor knockout mice show no obvious abnormalities in their development, survival or reproduction, and have normal platelet morphology and count.
However, they have inpaired platelet aggregation in response to ADP and other agonists, and resistance to thromboembolism.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  30
P2Y1 receptor deficiency resulted in a reduction of atherosclerosis in ApoE knockout mice.
Species:  Mouse
Tissue: 
Technique:  Gene targeting in embryonic stem cells.
References:  20
In vivo knockdown of the P2Y1 receptor by administration of short hairpin RNA selectively impairs the migration of neural progenitors to the subventricular zone
Species:  Mouse
Tissue: 
Technique:  RNAi
References:  33
P2Y1 knockout mice are protected from renal disease and resistant to capillary loss during passive crescentic glomerulonephritis
Species:  Mouse
Tissue: 
Technique:  Knockout by gene targeting in embryonic stem cells
References:  24
Phenotypes, Alleles and Disease Models Mouse data from MGI

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Allele Composition & genetic background Accession Phenotype Id Phenotype Reference
P2ry1tm1Gac P2ry1tm1Gac/P2ry1tm1Gac
involves: 129S2/SvPas * C57BL/6
MGI:105049  MP:0002551 abnormal blood coagulation PMID: 10606627 
P2ry1tm1Bhk P2ry1tm1Bhk/P2ry1tm1Bhk
involves: 129P2/OlaHsd * C57BL/6 * DBA/2
MGI:105049  MP:0005464 abnormal platelet physiology PMID: 10502826 
P2ry1tm1Bhk P2ry1tm1Bhk/P2ry1tm1Bhk
involves: 129P2/OlaHsd * C57BL/6 * DBA/2
MGI:105049  MP:0003422 abnormal thrombolysis PMID: 10502826 
P2ry1tm1Gac P2ry1tm1Gac/P2ry1tm1Gac
involves: 129S2/SvPas * C57BL/6
MGI:105049  MP:0009549 decreased platelet aggregation PMID: 10606627 
P2ry1+|P2ry1tm1Gac P2ry1tm1Gac/P2ry1+
involves: 129S2/SvPas * C57BL/6
MGI:105049  MP:0009549 decreased platelet aggregation PMID: 10606627 
P2ry1tm1Gac P2ry1tm1Gac/P2ry1tm1Gac
involves: 129S2/SvPas * C57BL/6
MGI:105049  MP:0005606 increased bleeding time PMID: 10606627 
P2ry1tm1Bhk P2ry1tm1Bhk/P2ry1tm1Bhk
involves: 129P2/OlaHsd * C57BL/6 * DBA/2
MGI:105049  MP:0005606 increased bleeding time PMID: 10502826 
Biologically Significant Variants
Type:  Single nucleotide polymorphism
Species:  Human
Description:  A silent polymorphism in the coding seguence of the P2Y1 gene is associated with different platelet reactivity to ADP
References:  23
Type:  Single nucleotide polymorphism
Species:  Human
Description:  The presence of a polymorphism appears to confer an attenuated antiplatelet effect during aspirin treatment in healthy Chinese subjects
References:  32
General Comments
In all species, the P2Y1 receptor is selective for adenine nucleotides. Presence of P2Y1 receptors has been reported in mitochondria of astrocytes and C6 cells, although its role in these sub-cellular structures remains unclear [29].
Available Assays
DiscoveRx PathHunter® U2OS P2RY1 β-Arrestin Cell Line (Cat no. 93-0941C3) more info

REFERENCES

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14. Filippov AK, Choi RC, Simon J, Barnard EA, Brown DA. (2006) Activation of P2Y1 nucleotide receptors induces inhibition of the M-type K+ current in rat hippocampal pyramidal neurons. J. Neurosci.26: 9340-9348. [PMID:16957090]

15. Fujita T, Tozaki-Saitoh H, Inoue K. (2009) P2Y1 receptor signaling enhances neuroprotection by astrocytes against oxidative stress via IL-6 release in hippocampal cultures. Glia57: 244-257. [PMID:18756525]

16. Gallagher CJ, Salter MW. (2003) Differential properties of astrocyte calcium waves mediated by P2Y1 and P2Y2 receptors. J Neurosci23: 6728-6839. [PMID:12890765]

17. Gao ZG, Mamedova L, Tchilibon S, Gross AS, Jacobson KA. (2004) 2,2'-Pyridylisatogen tosylate antagonizes P2Y1 receptor signaling without affecting nucleotide binding. Biochem Pharmacol.68: 231-237. [PMID:15193995]

18. Gao ZG, Mamedova LK, Chen P, Jacobson KA. (2004) 2-Substituted adenosine derivatives: affinity and efficacy at four subtypes of human adenosine receptors. Biochem Pharmacol68: 1985-1993. [PMID:15476669]

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20. Hechler B, Freund M, Ravanat C, Magnenat S, Cazenave JP, Gachet C. (2008) Reduced atherosclerotic lesions in P2Y1/apolipoprotein E double-knockout mice: the contribution of non-hematopoietic-derived P2Y1 receptors. Circulation118: 754-763. [PMID:18663083]

21. Hechler B, Leon C, Vial C, Vigne P, Frelin C, Cazenave JP, Gachet C. (1998) The P2Y1 receptor is necessary for adenosine 5'-diphosphate-induced platelet aggregation. Blood92: 152-159. [PMID:9639511]

22. Hechler B, Vigne P, Léon C, Breittmayer JP, Gachet C, Frelin C. (1998) ATP derivatives are antagonists of the P2Y1receptor: similarities to the platelet ADP receptor. Mol. Pharmacol.53: 727-733. [PMID:9547364]

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29. Krzeminski P, Misiewicz I, Pomorski P, Kasprzycka-Guttman T, Baranska J. (2007) Mitochondrial localization of P2Y1, P2Y2 and P2Y12 receptors in rat astrocytes and glioma C6 cells. Brain Res Bull71: 587-592. [PMID:17292801]

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38. Pfefferkorn JA, Choi C, Winters T, Kennedy R, Chi L, Perrin LA, Lu G, Ping YW, McClanahan T, Schroeder R et al.. (2008) P2Y1 receptor antagonists as novel antithrombotic agents. Bioorg. Med. Chem. Lett.18 (11): 3338-43. [PMID:18445527]

39. Ruan HZ, Burnstock G. (2003) Localisation of P2Y1 and P2Y4 receptors in dorsal root, nodose and trigeminal ganglia of the rat. Histochem Cell Biol120: 415-426. [PMID:14564529]

40. Ruel R, L'heureux A, Thibeault C, Daris JP, Martel A, Price LA, Wu Q, Hua J, Wexler RR, Rehfuss R et al.. (2013) New azole antagonists with high affinity for the P2Y1 receptor. Bioorg. Med. Chem. Lett.23 (12): 3519-22. [PMID:23668989]

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To cite this database page, please use the following:

Maria-Pia Abbracchio, Jean-Marie Boeynaems, José L. Boyer, Geoffrey Burnstock, Stefania Ceruti, Marta Fumagalli, Christian Gachet, Rebecca Hills, Robert G. Humphries, Kenneth A. Jacobson, Charles Kennedy, Brian F. King, Davide Lecca, Maria Teresa Miras-Portugal, Gary A. Weisman.
P2Y receptors: P2Y1 receptor. Last modified on 23/05/2014. Accessed on 27/08/2014. IUPHAR database (IUPHAR-DB), http://www.iuphar-db.org/DATABASE/ObjectDisplayForward?objectId=323.

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