Affinage

P2RX1

P2X purinoceptor 1 · UniProt P51575

Length
399 aa
Mass
45.0 kDa
Annotated
2026-04-29
100 papers in source corpus 39 papers cited in narrative 40 extracted findings

Mechanistic narrative

Synthesis pass · prose summary of the discoveries below

P2RX1 encodes an ATP-gated non-selective cation channel that assembles as a homotrimer or heteromerizes with P2X2, P2X4, or P2X5 subunits to form channels with distinct kinetic and pharmacological properties (PMID:9855626, PMID:15313628, PMID:15686495). The intersubunit ATP binding site is formed by residues K68, F185, F291, R292, and K309 from adjacent subunits, and ATP binding drives extensive extracellular domain rearrangements leading to fast channel opening followed by rapid desensitization that masks true nanomolar agonist affinity (PMID:14699168, PMID:17287520, PMID:12719485, PMID:22393010). Channel function depends on cholesterol-rich lipid raft localization mediated by N-terminal residues, direct PI(4,5)P2 binding at C-terminal K364, HSP90-dependent trafficking, and Gαq-GPCR signaling through phosphorylation of an accessory protein (PMID:16006561, PMID:20699225, PMID:18523136, PMID:22851178, PMID:15144237). Physiologically, P2X1 mediates sympathetic smooth muscle contraction in the vas deferens essential for male fertility, renal afferent arteriolar autoregulation via tubuloglomerular feedback, platelet shape change and thrombosis amplification through ERK2-MLCK signaling, and neutrophil chemotaxis and extravasation via RhoA-Rho kinase-dependent MLC phosphorylation (PMID:10638758, PMID:14679185, PMID:12913094, PMID:14500714, PMID:19635923, PMID:25150292).

Mechanistic history

Synthesis pass · year-by-year structured walk · 24 steps
  1. 1996 High

    Establishing that platelets express a functional P2X1 channel with fast activation/desensitization kinetics and Ca²⁺ permeability answered the basic question of what ATP receptor type mediates cation influx in platelets.

    Evidence Whole-cell patch clamp and Fura-2 Ca²⁺ imaging of human platelets

    PMID:8621673

    Open questions at the time
    • Physiological consequence of platelet P2X1 activation in hemostasis unknown
    • Molecular determinants of fast desensitization not identified
  2. 1998 High

    Demonstration that P2X1 can heteromerize with P2X5 to form channels with distinct kinetics (non-desensitizing plateau) established that P2X1 subunit composition diversifies purinergic signaling properties in native tissues.

    Evidence Co-expression in HEK293 and Xenopus oocytes with co-immunoprecipitation and electrophysiology; confirmed by reciprocal co-purification

    PMID:10336430 PMID:9855626

    Open questions at the time
    • Native tissues expressing P2X1/5 heteromers not yet identified
    • Stoichiometry of heteromeric assembly unknown
  3. 1998 Medium

    Revealing that actin cytoskeleton disruption alters P2X1 gating kinetics identified the cytoskeleton as a modulator of channel function, suggesting native channel behavior depends on cellular context beyond intrinsic subunit properties.

    Evidence Whole-cell patch clamp of HEK293 cells stably expressing P2X1 with cytochalasin B/D treatment and mutagenesis

    PMID:9625863

    Open questions at the time
    • Direct protein interaction between actin and P2X1 not demonstrated
    • Mechanism by which pore-region mutations uncouple cytoskeletal regulation unclear
  4. 2000 High

    The P2X1 knockout mouse revealed that the channel is essential for vas deferens contraction and male fertility, establishing the first definitive physiological role for P2X1 in vivo.

    Evidence Targeted gene deletion in mice with contractility and fertility assays

    PMID:10638758

    Open questions at the time
    • Whether P2X1 loss affects other smooth muscle beds not fully explored
    • Mechanism of reduced sperm in ejaculate not mechanistically dissected
  5. 2000 High

    Identification of a naturally occurring dominant-negative P2X1 mutant (TM2 leucine deletion) that reaches the surface but forms non-conducting channels demonstrated that the TM2 region is critical for pore function and that defective subunits can poison trimeric assemblies.

    Evidence Confocal localization and voltage clamp co-expression in Xenopus oocytes

    PMID:10816552

    Open questions at the time
    • Whether this variant exists in patients with unexplained phenotypes unknown
    • Structural basis of pore dysfunction not resolved
  6. 2002 High

    Showing that the conserved N-terminal T18 PKC site is essential for P2X1 gating (T18A reduces current >99%) defined a key regulatory phosphorylation event controlling channel amplitude and desensitization.

    Evidence Site-directed mutagenesis with two-electrode voltage clamp in Xenopus oocytes

    PMID:11855833

    Open questions at the time
    • Whether T18 phosphorylation is constitutive or dynamically regulated in native cells not shown
  7. 2003 High

    Systematic mutagenesis and intersubunit disulfide cross-linking defined the ATP binding pocket as an intersubunit site formed by K68, F185, F291, R292, and K309, resolving the long-standing question of how trimeric P2X channels bind ATP.

    Evidence Cysteine mutagenesis with cross-linking, alanine scanning, partial agonist analysis, and DTT rescue in Xenopus oocytes

    PMID:14699168 PMID:17287520

    Open questions at the time
    • Full atomic-resolution structure of ATP-bound P2X1 not available
    • Contribution of each residue to binding energy not quantified
  8. 2003 High

    Chimeric P2X2/P2X1 receptors revealed that P2X1 possesses true nanomolar ATP affinity (K₁/₂ ~3 nM for desensitization) that is masked by ultrafast desensitization, fundamentally reframing the channel's sensitivity and establishing a C→O→D linear gating model.

    Evidence Two-electrode voltage clamp with rapid solution exchange and chimeric receptors in Xenopus oocytes

    PMID:12719485 PMID:14625300

    Open questions at the time
    • Structural basis for the coupling between open state and desensitized state not resolved
  9. 2003 High

    P2X1 knockout and transgenic overexpression studies established that P2X1 drives platelet activation through an ERK2→MLCK→MLC phosphorylation axis, amplifying shape change, secretion, and thrombosis under arterial shear conditions.

    Evidence P2X1 KO and transgenic mice with aggregometry, flow chambers, in vivo thrombosis models, Western blot, and MEK inhibitor rescue

    PMID:12521992 PMID:12913094 PMID:14500714

    Open questions at the time
    • Whether ERK2-MLCK axis operates identically in human platelets in vivo not confirmed
    • Direct P2X1–ERK2 signaling intermediates not identified
  10. 2003 High

    P2X1 deletion impaired renal afferent arteriolar autoregulation and tubuloglomerular feedback, identifying P2X1 as the receptor coupling ATP released at the macula densa to preglomerular vasoconstriction.

    Evidence P2X1 KO mice and NF279 blockade with juxtamedullary nephron preparation and papillectomy/furosemide dissection

    PMID:14679185

    Open questions at the time
    • Source of ATP mediating tubuloglomerular feedback not definitively identified
    • Whether P2X1 heteromers contribute to renal autoregulation not tested
  11. 2004 High

    Blue native PAGE confirmed P2X1 assembles as trimers and forms heterotrimers with P2X2, resolving the stoichiometry question for the P2X receptor family.

    Evidence Blue native PAGE and SDS-PAGE of P2X1 and multiple P2X subtypes expressed in Xenopus oocytes

    PMID:15313628

    Open questions at the time
    • Subunit arrangement within heterotrimers (e.g., 2:1 vs. 1:2) not determined
  12. 2004 High

    Gαq-GPCR potentiation of P2X1 was shown to act not through direct channel phosphorylation at T18 but through PKC-dependent phosphorylation of an unidentified accessory protein, revealing an indirect regulatory mechanism.

    Evidence Co-expression in oocytes, T18A mutagenesis, PLC/PKC inhibitors, ³²P radiolabeling in HEK293

    PMID:15144237

    Open questions at the time
    • Identity of the accessory protein mediating GPCR potentiation remains unknown
  13. 2005 High

    Demonstration that P2X1 resides in lipid rafts and that cholesterol depletion abolishes >90% of P2X1 current established lipid raft integrity as essential for channel function in smooth muscle and recombinant systems.

    Evidence Sucrose gradient fractionation, patch clamp, and rat tail artery contractility with methyl-β-cyclodextrin

    PMID:16006561

    Open questions at the time
    • Direct cholesterol–P2X1 interaction site not mapped at this stage
  14. 2008 High

    PI(4,5)P₂ was identified as a direct lipid modulator of P2X1, with K364 in the C-terminus mediating binding; inside-out patch rescue with exogenous PI(4,5)P₂ established this as a direct gating requirement.

    Evidence Inside-out macropatch recording with PI(4,5)P₂ application, wortmannin depletion, K364 mutagenesis, binding assay

    PMID:18523136

    Open questions at the time
    • Whether PI(4,5)P₂ modulates heteromeric P2X1-containing channels similarly untested
  15. 2008 Medium

    P2X1/P2X5 heteromers were identified as the predominant functional ATP receptor in cortical astrocytes, providing the first strong evidence for a native P2X1-containing heteromer in a specific cell type.

    Evidence Whole-cell voltage clamp of acutely isolated GFAP-eGFP+ astrocytes with pharmacological profiling and qRT-PCR

    PMID:18495881

    Open questions at the time
    • Heteromeric identity inferred pharmacologically, not confirmed by subunit-selective deletion
    • Single laboratory observation
  16. 2009 High

    P2X1 was shown to drive neutrophil chemotaxis via a RhoA→Rho kinase→MLC axis controlling trailing-edge retraction, establishing an innate immune function for P2X1 beyond hemostasis.

    Evidence P2X1 KO neutrophil chemotaxis, RhoA pull-down, MLC phosphorylation, Rho kinase inhibitors, in vivo peritoneal recruitment

    PMID:19635923

    Open questions at the time
    • How P2X1-derived Ca²⁺ signal activates RhoA specifically at the uropod not determined
  17. 2010 High

    Cholesterol sensitivity was mapped to N-terminal residues 20–29 of P2X1 using chimeras and point mutations, and was shown to affect gating rather than ATP affinity or surface expression, resolving the mechanism of lipid raft dependence.

    Evidence P2X1/P2X2 chimeras, point mutagenesis, patch clamp in HEK293 with cholesterol depletion

    PMID:20699225

    Open questions at the time
    • Whether these residues directly bind cholesterol or interact with a raft-associated protein undetermined
  18. 2010 High

    FRAP and pharmacological trafficking inhibitors showed that P2X1 undergoes agonist-stimulated lateral mobility and dynamin-dependent internalization/recycling, linking receptor trafficking to recovery from desensitization.

    Evidence FRAP of P2X1-eGFP in HEK293 with brefeldin A and dynasore treatment

    PMID:20374431

    Open questions at the time
    • Recycling compartment identity not determined
    • Whether agonist-driven internalization involves ubiquitination not tested
  19. 2010 High

    P2X1 (with P2X4) was found to translocate to the immune synapse upon TCR stimulation, where pannexin-1-released ATP activates these channels to drive NFAT-dependent IL-2 production, establishing an autocrine purinergic loop in T cell activation.

    Evidence Confocal imaging, siRNA knockdown, Ca²⁺ imaging, NFAT reporter, and IL-2 ELISA in T cells

    PMID:20660288

    Open questions at the time
    • Relative contributions of P2X1 vs. P2X4 to T cell Ca²⁺ entry not separated
    • Whether P2X1/P2X4 heteromers form at the immune synapse not tested
  20. 2012 High

    Voltage clamp fluorometry and accessibility mapping revealed that ATP binding induces propeller-head domain rotation, intersubunit sliding, and lateral portal rearrangement, with specific residues reporting activation versus desensitization conformational transitions.

    Evidence VCF with cysteine-TMRM labeling, MTSEA-biotinylation, EM, and disulfide cross-linking in Xenopus oocytes

    PMID:22393010 PMID:22745172

    Open questions at the time
    • Full high-resolution structure of P2X1 in open and desensitized states not solved
  21. 2012 High

    HSP90 was identified as required for P2X1 surface trafficking and lateral mobility, with inhibitors reducing surface expression by ~70–85% and platelet P2X1-mediated Ca²⁺ entry by ~40–45%; sensitivity mapped to intracellular termini.

    Evidence Geldanamycin/radicicol treatment with patch clamp, photoactivatable-GFP imaging, chimeric mapping, and platelet Ca²⁺ assay

    PMID:22851178

    Open questions at the time
    • Direct HSP90–P2X1 binding site not mapped
    • Whether HSP90 acts as a foldase or trafficking escort not distinguished
  22. 2013 High

    Double knockout of α1A-adrenoceptors and P2X1 produced 100% male infertility by eliminating sympathetic vas deferens contraction, establishing that these two receptor systems are non-redundantly required and together fully account for sympathetic ejaculatory function.

    Evidence α1A-AR × P2X1 double knockout mice with fertility testing and ICSI rescue

    PMID:24297884

    Open questions at the time
    • Whether pharmacological dual blockade reproduces the contraceptive phenotype in other species not tested
  23. 2014 High

    P2X1-mediated Ca²⁺ influx was shown to potentiate P2Y1-evoked Ca²⁺ signals superadditively via IP3 receptor/PLC amplification, providing a molecular mechanism for how transient P2X1 activation can have lasting effects on platelet aggregation.

    Evidence Ca²⁺ imaging in platelets and HEK293 with selective P2X1/P2Y1 pharmacology, ionomycin mimicry, and inhibitor panel

    PMID:24923466

    Open questions at the time
    • Whether Ca²⁺ potentiates PLC directly or acts through an intermediate kinase not resolved
  24. 2014 High

    Adoptive transfer experiments demonstrated that neutrophil P2X1 (not platelet P2X1 alone) is required for thrombus formation and neutrophil extravasation during inflammation, redefining P2X1 as a critical innate immune effector in thromboinflammation.

    Evidence P2X1 KO mice with intravital microscopy, labeled neutrophil/platelet adoptive transfer, fibrin assays, and LPS endotoxemia model

    PMID:25150292 PMID:25480563

    Open questions at the time
    • Molecular events downstream of neutrophil P2X1 activation that promote fibrin generation not fully characterized

Open questions

Synthesis pass · forward-looking unresolved questions
  • Key unresolved questions include the identity of the accessory protein mediating GPCR potentiation, the high-resolution structure of P2X1 in distinct gating states, and the mechanisms by which P2X1 couples to RhoA in neutrophils and modulates IP3R/PLC in platelets.
  • Accessory protein for Gαq potentiation unidentified
  • No high-resolution P2X1 structure in open or desensitized state
  • Coupling mechanism from P2X1 Ca²⁺ entry to RhoA activation in neutrophils not determined

Mechanism profile

Synthesis pass · controlled-vocabulary classification · explore literature graph →
Molecular activity
GO:0005215 transporter activity 6 GO:0008289 lipid binding 1
Localization
GO:0005886 plasma membrane 7 GO:0031410 cytoplasmic vesicle 1
Pathway
R-HSA-162582 Signal Transduction 5 R-HSA-168256 Immune System 4 R-HSA-382551 Transport of small molecules 4 R-HSA-109582 Hemostasis 3 R-HSA-397014 Muscle contraction 3 R-HSA-1474165 Reproduction 2
Partners
ADRA1AHSP90P2RX2P2RX4P2RX5P2RY1
Complex memberships
P2X1 homotrimerP2X1/P2X2 heteromerP2X1/P2X4 heteromerP2X1/P2X5 heteromer

Evidence

Reading pass · 40 per-paper findings extracted from the source corpus
Year Finding Method Journal Conf PMIDs
2000 P2X1 receptor is essential for normal vas deferens contraction and male reproductive function; P2X1 knockout mice show ~60% reduction in vas deferens contraction to sympathetic nerve stimulation and ~90% reduction in male fertility due to reduced sperm in ejaculate. Targeted gene deletion (knockout mice), contractility assays, fertility studies Nature High 10638758
1996 P2X1 receptors in human platelets function as rapidly activating (within 20 ms), rapidly desensitizing (time constant 47–107 ms) cation channels (11 pS single-channel conductance) permeable to monovalent and divalent cations, activated by ATP, ADP, and non-hydrolyzable ATP analogues, mediating Ca2+ influx distinct from intracellular store release. Whole-cell patch clamp (nystatin perforated patch), Fura-2 Ca2+ imaging The Journal of biological chemistry High 8621673
2003 P2X1 receptors mediate pressure-induced afferent arteriolar autoregulatory vasoconstriction in the kidney; deletion of P2X1 or blockade with NF279 blunts autoregulatory responses to renal perfusion pressure increases, and tubuloglomerular feedback signals are coupled to preglomerular vasoconstriction through ATP-mediated P2X1 activation. P2X1 KO mice, juxtamedullary nephron preparation, pharmacological blockade (NF279, DPCPX), papillectomy/furosemide to dissect tubuloglomerular feedback The Journal of clinical investigation High 14679185
2003 P2X1 receptors play a role in arterial thrombosis in vivo; P2X1-deficient mice show reduced collagen-induced platelet aggregation, decreased thrombus growth on collagen-coated surfaces at high shear rates, reduced mortality in systemic thromboembolism, and smaller laser-induced mural thrombi. P2X1 KO mice, in vitro aggregation assays, flow chamber experiments, in vivo thrombosis models (thromboembolism, laser injury) The Journal of experimental medicine High 12913094
2003 P2X1 receptor overexpression in platelets enhances Ca2+ influx, platelet shape change, secretion, and aggregation to collagen and convulxin, and upregulates ERK2 phosphorylation; MEK1/2 inhibition abolishes P2X1-dependent platelet hyperreactivity and protects against thromboembolism in vivo. Transgenic mouse overexpressing human P2X1 in megakaryocytes, Ca2+ imaging, aggregometry, flow chamber, Western blot, in vivo thromboembolism model, MEK inhibitor U0126 Blood High 12521992
2003 P2X1 activation in platelets induces ERK2 phosphorylation, which amplifies collagen-induced platelet secretion by reinforcing myosin light chain kinase (MLCK) activation; Ca2+/calmodulin-dependent MLCK (not Rho kinase) mediates P2X1-evoked MLC phosphorylation and shape change. Transmission electron microscopy, Western blot for MLC and ERK2 phosphorylation, pharmacological inhibitors (W-7, ML-7, HA-1077, U0126, GF109203-X, PP1), P2X1 desensitization experiments The Journal of biological chemistry High 14500714
1998 P2X1 and P2X5 subunits co-assemble to form a novel heteromeric ATP-gated ion channel with distinct biophysical properties (biphasic current with non-desensitizing plateau, higher EC50 for αβ-methylene ATP) distinct from either homomeric channel; heteromeric assembly confirmed biochemically. Co-expression in HEK293 cells, whole-cell patch clamp, co-immunoprecipitation of epitope-tagged subunits Molecular pharmacology High 9855626
1999 Rat P2X1 and P2X5 subunits form heteromeric ATP-gated channels with the pharmacology of P2X1 (high αβ-methylene ATP sensitivity, nanomolar TNP-ATP antagonism) and the slow desensitization kinetics of P2X5; physical co-assembly demonstrated by reciprocal co-purification. Xenopus oocyte expression, two-electrode voltage clamp, reciprocal co-purification of epitope-tagged subunits from HEK293 cells The Journal of biological chemistry High 10336430
2004 P2X receptors, including P2X1 and P2X2, are assembled as homotrimers or heterotrimers; trimeric architecture is demonstrated biochemically for P2X1 and multiple P2X subtypes; co-expressed P2X1 and P2X2 subunits form heterotrimers exported to the plasma membrane. Blue native PAGE, SDS-PAGE, biochemical size analysis, Xenopus oocyte expression Journal of molecular biology High 15313628
2005 P2X1 and P2X4 subunits form heteromeric trimeric receptors with kinetics resembling homomeric P2X4 but pharmacology similar to homomeric P2X1 (sensitivity to αβ-meATP, suramin, TNP-ATP); heteromerization confirmed by co-purification and blue native PAGE. Xenopus oocyte co-injection, two-electrode voltage clamp, co-purification of His-tagged subunits, blue native PAGE Journal of neurochemistry High 15686495
2003 The ATP binding site of P2X1 is formed at the interface between neighboring subunits; intersubunit disulfide cross-links form spontaneously between K68C and F291C mutants, indicating these residues from adjacent subunits are in close proximity in the ATP binding pocket. Disulfide cross-linking, non-reducing SDS-PAGE, cysteine mutagenesis, two-electrode voltage clamp in Xenopus oocytes, dithiothreitol rescue The Journal of neuroscience High 17287520
2003 Basic residues Lys-68, Phe-185, Phe-291, Arg-292, and Lys-309 contribute to ATP binding at the P2X1 receptor; Phe-185 and Phe-291 coordinate the adenine ring of ATP, while Lys-68, Arg-292, and Lys-309 are critical for agonist binding as revealed by partial agonist analysis. Alanine substitution mutagenesis, two-electrode voltage clamp in Xenopus oocytes, partial agonist (BzATP, Ap5A) analysis The Journal of biological chemistry High 14699168
2005 P2X1 receptors are localized in cholesterol-rich lipid rafts in smooth muscle and recombinant expression systems; disruption of lipid rafts by methyl-β-cyclodextrin redistributes P2X1 and reduces P2X1-mediated currents by >90% and arterial contractions by ~50%, demonstrating functional dependence on lipid raft association. Discontinuous sucrose density gradient fractionation, Western blot, cholesterol measurement, patch clamp (HEK293), contractility assay (rat tail artery), methyl-β-cyclodextrin cholesterol depletion The Journal of biological chemistry High 16006561
2010 Cholesterol sensitivity of P2X1 (but not P2X2-4) receptors is mediated through intracellular amino-terminal residues (positions 20-23 and 27-29) between the PKC site and TM1; cholesterol is required for channel gating rather than ATP sensitivity or surface expression. Chimeric receptor construction (P2X1/P2X2), point mutagenesis, patch clamp in HEK293, methyl-β-cyclodextrin and filipin treatment, lipid raft fractionation The Journal of biological chemistry High 20699225
2004 GPCR-mediated potentiation of P2X1 receptors does not involve direct phosphorylation of the channel at the conserved PKC site (T18); instead, potentiation by Gαq-coupled receptors and phorbol esters is blocked by staurosporine and likely acts through phosphorylation of an accessory protein in the P2X1 receptor complex. Co-expression in Xenopus oocytes, mutagenesis (T18A PKC site), PLC inhibitor (U-73122), PKC inhibitors, BAPTA chelation, 32P radiolabeling of phosphorylated proteins in HEK293 The Biochemical journal High 15144237
2008 Phosphatidylinositol 4,5-bisphosphate (PI(4,5)P2) directly modulates P2X1 channel function; depletion of PI(4,5)P2 decreases P2X1 current amplitude and recovery; the proximal C-terminal region (Lys364 identified as critical) directly binds PI(4,5)P2, and direct application to inside-out patches rescues currents from rundown. Xenopus oocyte electrophysiology, wortmannin treatment, isolated mesenteric artery contraction assay, inside-out macropatch recording with exogenous PI(4,5)P2, mutagenesis (K364), biochemical binding assay Molecular pharmacology High 18523136
2009 P2X1 ion channels promote neutrophil chemotaxis through RhoA GTPase activation and Rho kinase-dependent myosin light chain phosphorylation at the cell rear; P2X1-deficient neutrophils show impaired chemotaxis, reduced speed, and defective trailing edge retraction. Patch clamp of human and mouse neutrophils, P2X1 KO mice, Boyden chamber chemotaxis assay, RhoA activation assay, MLC phosphorylation, Rho kinase inhibitors (Y27632, H1152), in vivo peritoneal recruitment (E. coli) Journal of immunology High 19635923
2010 TCR stimulation induces translocation of P2X1 (and P2X4) receptors and pannexin-1 hemichannels to the immune synapse; pannexin-1 mediates ATP release, and P2X1/P2X4 activation drives Ca2+ entry, NFAT activation, and IL-2 synthesis in T cells as part of an autocrine feedback loop. Confocal microscopy (receptor translocation), siRNA silencing, pharmacological inhibition, Ca2+ imaging, NFAT reporter assay, IL-2 ELISA Blood High 20660288
2000 A naturally occurring dominant negative P2X1 mutant lacking one leucine in TM2 (L351-354 region) localizes correctly to the plasma membrane but forms non-conducting channels and exerts dose-dependent dominant negative suppression of wild-type P2X1 current when co-expressed. Confocal microscopy (HEK293 stable transfection), voltage clamp in Xenopus oocytes, co-expression with WT receptor The Journal of biological chemistry High 10816552
2002 The conserved N-terminal PKC site (T18) is critical for P2X1 gating; T18A mutation reduces peak current by >99% and accelerates desensitization ~10-fold; co-expression data show T18A dominates the desensitization phenotype in heteromeric channels. Xenopus oocyte expression, two-electrode voltage clamp, mutagenesis, co-expression dose-response Biochemical and biophysical research communications High 11855833
2012 The cysteine-rich head domain of P2X1 undergoes conformational movements during activation and desensitization; fluorescent labeling of cysteine mutants reveals fast movements correlated with activation (N120C, G123C) and slow movements correlated with desensitization (P121C, I125C); TNP-ATP induces large fluorescence changes, confirming proximity to the ATP binding site. Voltage clamp fluorometry, cysteine mutagenesis, TMRM labeling, Xenopus oocyte expression, molecular modeling Proceedings of the National Academy of Sciences of the United States of America High 22745172
2012 ATP binding induces extensive conformational rearrangement of the P2X1 extracellular domain including propeller-head domain rotation, sliding of adjacent subunits restricting upper vestibule access, and movement in lateral portals; disulfide bonds restricting intersubunit movements inhibit channel function. MTSEA-biotinylation accessibility mapping, homology model, electron microscopy of purified P2X1, disulfide crosslinking between subunits Proceedings of the National Academy of Sciences of the United States of America High 22393010
2012 Positively charged residues in the cysteine-rich head region (Lys111, Lys127, Lys138, Lys148; particularly K138) account for selective antagonism by NF449 and suramin at human P2X1 versus P2X2 receptors; chimeras replacing this region reduce NF449 sensitivity ~1000-fold. Chimeric receptor construction (P2X1/P2X2), point mutagenesis, two-electrode voltage clamp in Xenopus oocytes British journal of pharmacology High 21671897
2010 P2X1 receptors undergo lateral membrane mobility and recycling; receptor activation by αβ-methylene ATP doubles the FRAP recovery rate; brefeldin A (blocking exocytic trafficking) and dynasore (blocking dynamin-dependent endocytosis after activation) impair recovery from desensitization. FRAP of P2X1-eGFP in HEK293 cells, brefeldin A and dynasore treatment, cycloheximide protein synthesis inhibition, functional desensitization recovery assays Journal of neurochemistry High 20374431
1998 The actin cytoskeleton modulates P2X1 receptor activation and desensitization kinetics; treatment with cytochalasins B or D reverts native-like slow kinetics to rapid kinetics, implicating actin in supporting native channel gating; two point mutations in the pore region near TM2 prevent this cytoskeletal regulation. Whole-cell patch clamp of stably expressed P2X1 in HEK293, cytochalasin B/D treatment, morphological correlation with kinetic changes, mutagenesis The Journal of physiology Medium 9625863
2012 HSP90 is required for normal P2X1 receptor trafficking and function; selective HSP90 inhibitors (geldanamycin, radicicol) reduce P2X1 surface expression and currents by ~70-85%, abolish receptor mobility in real-time imaging of photoactivatable-GFP tagged receptors, and reduce platelet P2X1-mediated Ca2+ increases by 40-45%; sensitivity maps to intracellular N and C termini. Patch clamp (HEK293), photoactivatable GFP real-time imaging, chimeric receptor mapping, platelet Ca2+ imaging, geldanamycin/radicicol treatment The Journal of biological chemistry High 22851178
2003 The P2X1 receptor desensitizes at nanomolar ATP concentrations (K1/2 ~3.2 nM for desensitization vs. EC50 ~0.7 µM for activation); true nanomolar agonist affinity is masked by fast desensitization; desensitization occurs exclusively via the open conformation consistent with a C-O-D linear model. Two-electrode voltage clamp in Xenopus oocytes, P2X2/P2X1 chimera to unmask steady-state responses, rapid solution exchange system The Journal of general physiology High 12719485
2003 The P2X1 ectodomain confers nanomolar ATP sensitivity (EC50 ~3.3 nM via P2X2/P2X1 chimera) that is obscured by fast desensitization in the wild-type receptor; deactivation time constants reflect unbinding rates and define true agonist potency. Two-electrode voltage clamp in Xenopus oocytes, P2X2/P2X1 chimera with full P2X1 ectodomain, agonist concentration-response analysis The Journal of biological chemistry High 14625300
2014 P2X1 expressed on neutrophils (not platelets alone) is required for thrombosis; absence of P2X1 on neutrophils impairs their adhesion and activation at sites of endothelial injury, reducing fibrin generation; restoration of thrombosis requires infusion of both WT platelets and WT neutrophils into P2X1-deficient mice. P2X1 KO mice, adoptive transfer of labeled neutrophils/platelets, intravital microscopy, fibrin generation assay, in vitro PMN activation assays Blood High 25150292
2014 P2X1 receptor is required for neutrophil emigration from venules during LPS-induced endotoxemia; P2X1-deficient mice show reduced neutrophil accumulation in lungs, less tissue damage, reduced coagulation activation, lower cytokine/chemokine levels, and resistance to LPS-induced death; adoptive transfer shows the defect is intrinsic to neutrophils. P2X1 KO mice, intravital microscopy (cremaster venules), adoptive transfer of fluorescent neutrophils, cytokine ELISA, coagulation assays Journal of immunology High 25480563
2013 Simultaneous knockout of α1A-adrenoceptors and P2X1 receptors in male mice produces 100% infertility by blocking sympathetically mediated sperm transport through the vas deferens during ejaculatory emission, without affecting sexual behavior, sperm quality, or fertility when sperm are harvested and used for ICSI. Double knockout mice (α1A-AR × P2X1), fertility testing, sperm quality assessment, ICSI, blood pressure measurement Proceedings of the National Academy of Sciences of the United States of America High 24297884
2014 Ca2+ influx through P2X1 receptors amplifies P2Y1-evoked Ca2+ signaling via potentiation of IP3 receptors and/or phospholipase C, resulting in superadditive Ca2+ increase; this potentiation is dependent on Ca2+ influx (not Na+ influx or depolarization), persists up to 60 s after P2X1 activation, and amplifies ADP-evoked platelet aggregation. Ca2+ imaging in human platelets and HEK293 cells, selective P2X1/P2Y1 pharmacology, ionomycin mimicry, PKC/ROCK/ERK inhibitors, aggregometry Molecular pharmacology High 24923466
2001 P2X1 receptor-mediated Ca2+ influx synergizes with P2Y receptor-mediated responses in platelets; co-application of αβ-meATP and ADP causes marked acceleration and amplification of the peak Ca2+ response; in megakaryocytes, P2Y-stimulated cation currents are reduced ~50% in P2X1-deficient mice, suggesting membrane conductance interaction. P2X1 KO mice, whole-cell patch clamp of megakaryocytes, Fura-2 Ca2+ imaging of human platelets, co-agonist stimulation protocols British journal of pharmacology High 11815371
2008 P2X1 and P2X5 subunits form the predominant functional ATP receptor in mouse cortical astrocytes; the receptor has high ATP sensitivity (EC50 ~40 nM), biphasic kinetics, and PPADS sensitivity matching heterologously expressed P2X1/5 heteromers; P2X1 and P2X5 mRNAs are the major P2X transcripts in these cells. Whole-cell voltage clamp of acutely isolated astrocytes from GFAP-eGFP transgenic mice, pharmacological characterization (PPADS, ivermectin), quantitative RT-PCR The Journal of neuroscience Medium 18495881
1998 P2X1 receptors are present in cholesterol-rich lipid rafts on smooth muscle; P2X1 receptor protein co-localizes with the lipid raft markers flotillin-1 and -2 in discontinuous sucrose density gradient fractions from smooth muscle tissues. Sucrose density gradient fractionation, Western blot, cholesterol measurement from smooth muscle (rat tail artery, vas deferens, bladder) and HEK293 The Journal of biological chemistry High 16006561
2021 P2RX1 deficiency in neutrophils upregulates Nrf2, which drives increased PD-L1 expression and metabolic reprogramming (enhanced mitochondrial metabolism); P2RX1 activation promotes platelets to release ATP, which supports neutrophil glycolytic metabolism and NETs formation during renal ischemia-reperfusion injury. P2rx1-/- mice, RNA sequencing, mitochondrial morphology assessment, neutrophil-platelet metabolic interaction assays, Nrf2/PD-L1 Western blot, NETs quantification Pharmacological research Medium 34091010
2014 Extracellular ATP induces intracellular alpha-synuclein accumulation via P2X1 receptor-mediated lysosomal dysfunction (elevation of lysosomal pH); Ca2+ influx through P2X1 is necessary but not sufficient alone for alpha-synuclein accumulation. Neuronal cell models, pharmacological P2X1 inhibition, lysosomal pH measurement, Ca2+ influx assays, alpha-synuclein immunoblot Neurobiology of aging Medium 25480524
2008 Ectodomain lysine K138 (human P2X1) is a key determinant for binding of both suramin and NF449; substitution K138E markedly reduces antagonist sensitivity, and introducing K138 into the mouse P2X1 receptor (where E138 is present) greatly increases sensitivity to suramin and NF449. Mutagenesis of human P2X1 and mouse P2X1 expressed in HEK293, whole-cell patch clamp ATP-evoked current inhibition The Journal of biological chemistry High 18765669
1998 Human P2X1 receptor is expressed on platelets as a ~60 kDa protein (reducing to ~46 kDa after endoglycosidase-F treatment, indicating N-glycosylation); P2X1 receptor-mediated ion fluxes are pharmacologically distinct from ADP receptor-mediated responses in human platelets. Immunoblot, endoglycosidase-F treatment, Ca2+ influx/mobilization assays, immunofluorescence Blood High 9558372
1998 P2X1 receptors in smooth muscle are localized in clusters directly apposed beneath sympathetic nerve varicosities; large clusters (~1.2 µm) are found under varicosities while small clusters (~0.4 µm) are not associated with varicosities. Immunofluorescence and confocal microscopy of rat urinary bladder smooth muscle with anti-P2X1 and anti-SV2 antibodies, 3D reconstruction Journal of neurocytology Medium 11246492

Source papers

Stage 0 corpus · 100 papers · ranked by NIH iCite citations
Year Title Journal Citations PMID
2000 Reduced vas deferens contraction and male infertility in mice lacking P2X1 receptors. Nature 310 10638758
2010 Pannexin-1 hemichannel-mediated ATP release together with P2X1 and P2X4 receptors regulate T-cell activation at the immune synapse. Blood 268 20660288
1998 Trinitrophenyl-substituted nucleotides are potent antagonists selective for P2X1, P2X3, and heteromeric P2X2/3 receptors. Molecular pharmacology 226 9614197
2005 Dual presynaptic control by ATP of glutamate release via facilitatory P2X1, P2X2/3, and P2X3 and inhibitory P2Y1, P2Y2, and/or P2Y4 receptors in the rat hippocampus. The Journal of neuroscience : the official journal of the Society for Neuroscience 187 16000618
2003 A role of the fast ATP-gated P2X1 cation channel in thrombosis of small arteries in vivo. The Journal of experimental medicine 175 12913094
1996 Activation of receptor-operated cation channels via P2X1 not P2T purinoceptors in human platelets. The Journal of biological chemistry 168 8621673
2008 P2X1 and P2X5 subunits form the functional P2X receptor in mouse cortical astrocytes. The Journal of neuroscience : the official journal of the Society for Neuroscience 142 18495881
2003 Physiological role for P2X1 receptors in renal microvascular autoregulatory behavior. The Journal of clinical investigation 141 14679185
1998 Co-expression of P2X1 and P2X5 receptor subunits reveals a novel ATP-gated ion channel. Molecular pharmacology 112 9855626
2001 Platelet shape change evoked by selective activation of P2X1 purinoceptors with alpha,beta-methylene ATP. Thrombosis and haemostasis 111 11246552
2003 Overexpression of the platelet P2X1 ion channel in transgenic mice generates a novel prothrombotic phenotype. Blood 108 12521992
2004 Trimeric architecture of homomeric P2X2 and heteromeric P2X1+2 receptor subtypes. Journal of molecular biology 99 15313628
2021 Identification of a subset of immunosuppressive P2RX1-negative neutrophils in pancreatic cancer liver metastasis. Nature communications 98 33420030
2004 Structure-activity relationships of analogues of NF449 confirm NF449 as the most potent and selective known P2X1 receptor antagonist. European journal of medicinal chemistry 90 15072843
2005 Disruption of lipid rafts inhibits P2X1 receptor-mediated currents and arterial vasoconstriction. The Journal of biological chemistry 87 16006561
2003 ATP binding at human P2X1 receptors. Contribution of aromatic and basic amino acids revealed using mutagenesis and partial agonists. The Journal of biological chemistry 86 14699168
1998 Coexpression of mRNAs for P2X1, P2X2 and P2X4 receptors in rat vascular smooth muscle: an in situ hybridization and RT-PCR study. Journal of vascular research 85 9647332
2007 Identification of an intersubunit cross-link between substituted cysteine residues located in the putative ATP binding site of the P2X1 receptor. The Journal of neuroscience : the official journal of the Society for Neuroscience 82 17287520
2009 Functional evidence for the expression of P2X1, P2X4 and P2X7 receptors in human lung mast cells. British journal of pharmacology 80 19552691
2005 Biochemical and functional evidence for heteromeric assembly of P2X1 and P2X4 subunits. Journal of neurochemistry 79 15686495
1997 Presence of P2X1 purinoceptors in human platelets and megakaryoblastic cell lines. Thrombosis and haemostasis 77 9423802
2009 P2X1 ion channels promote neutrophil chemotaxis through Rho kinase activation. Journal of immunology (Baltimore, Md. : 1950) 76 19635923
2001 The ATP-gated P2X1 ion channel acts as a positive regulator of platelet responses to collagen. Thrombosis and haemostasis 75 11816716
1999 Functional and biochemical evidence for heteromeric ATP-gated channels composed of P2X1 and P2X5 subunits. The Journal of biological chemistry 75 10336430
1999 Diinosine pentaphosphate (IP5I) is a potent antagonist at recombinant rat P2X1 receptors. British journal of pharmacology 74 10556935
2001 Distribution of P2X(1) and P2X(3) receptors in the rat and human urinary bladder. Pharmacology 73 11490205
2000 The suramin analogue NF279 is a novel and potent antagonist selective for the P2X(1) receptor. Neuropharmacology 73 10963748
1998 P2X1 purinoceptor in human platelets. Molecular cloning and functional characterization after heterologous expression. The Journal of biological chemistry 73 9565569
1996 P2X1 receptor activation in HL60 cells. Blood 70 8639881
2003 Desensitization masks nanomolar potency of ATP for the P2X1 receptor. The Journal of biological chemistry 68 14625300
2002 A study of P2X1 receptor function in murine megakaryocytes and human platelets reveals synergy with P2Y receptors. British journal of pharmacology 67 11815371
2014 P2X1 expressed on polymorphonuclear neutrophils and platelets is required for thrombosis in mice. Blood 64 25150292
2001 Structure-activity relationships of pyridoxal phosphate derivatives as potent and selective antagonists of P2X1 receptors. Journal of medicinal chemistry 64 11462975
2003 Activation and desensitization of the recombinant P2X1 receptor at nanomolar ATP concentrations. The Journal of general physiology 62 12719485
2005 Profiling at recombinant homomeric and heteromeric rat P2X receptors identifies the suramin analogue NF449 as a highly potent P2X1 receptor antagonist. Neuropharmacology 61 15721178
2001 NF449: a subnanomolar potency antagonist at recombinant rat P2X1 receptors. Naunyn-Schmiedeberg's archives of pharmacology 60 11521173
1999 Properties of the novel ATP-gated ionotropic receptor composed of the P2X(1) and P2X(5) isoforms. Molecular pharmacology 60 10496954
1998 The P2X1 receptor, an adenosine triphosphate-gated cation channel, is expressed in human platelets but not in human blood leukocytes. Blood 60 9558372
2004 G-protein-coupled receptor regulation of P2X1 receptors does not involve direct channel phosphorylation. The Biochemical journal 59 15144237
2003 P2X1-mediated ERK2 activation amplifies the collagen-induced platelet secretion by enhancing myosin light chain kinase activation. The Journal of biological chemistry 59 14500714
2000 Expression of purinergic receptors (ionotropic P2X1-7 and metabotropic P2Y1-11) during myeloid differentiation of HL60 cells. Biochimica et biophysica acta 58 11004484
2004 Emerging roles for P2X1 receptors in platelet activation. Platelets 57 15203715
2003 NF449, a novel picomolar potency antagonist at human P2X1 receptors. European journal of pharmacology 57 12787824
2012 Involvement of the cysteine-rich head domain in activation and desensitization of the P2X1 receptor. Proceedings of the National Academy of Sciences of the United States of America 56 22745172
2003 Monomeric and dimeric byproducts are the principal functional elements of higher order P2X1 concatamers. Molecular pharmacology 53 12488557
2012 Agonist binding evokes extensive conformational changes in the extracellular domain of the ATP-gated human P2X1 receptor ion channel. Proceedings of the National Academy of Sciences of the United States of America 50 22393010
2004 Renal autoregulation in P2X1 knockout mice. Acta physiologica Scandinavica 50 15283757
2000 A natural dominant negative P2X1 receptor due to deletion of a single amino acid residue. The Journal of biological chemistry 50 10816552
1999 Increase in cardiac P2X1-and P2Y2-receptor mRNA levels in congestive heart failure. Life sciences 50 10503935
2011 The P2X1 receptor and platelet function. Purinergic signalling 48 21484087
2005 Interplay between P2Y(1), P2Y(12), and P2X(1) receptors in the activation of megakaryocyte cation influx currents by ADP: evidence that the primary megakaryocyte represents a fully functional model of platelet P2 receptor signaling. Blood 48 15914557
2002 Sensitization by extracellular Ca(2+) of rat P2X(5) receptor and its pharmacological properties compared with rat P2X(1). Molecular pharmacology 48 12237343
2007 Primary and secondary agonists can use P2X(1) receptors as a major pathway to increase intracellular Ca(2+) in the human platelet. Journal of thrombosis and haemostasis : JTH 46 17362227
1998 A pyridoxine cyclic phosphate and its 6-azoaryl derivative selectively potentiate and antagonize activation of P2X1 receptors. Journal of medicinal chemistry 46 9632352
2010 Lipid raft association and cholesterol sensitivity of P2X1-4 receptors for ATP: chimeras and point mutants identify intracellular amino-terminal residues involved in lipid regulation of P2X1 receptors. The Journal of biological chemistry 45 20699225
2007 P2X1 and P2X4 receptor currents in mouse macrophages. British journal of pharmacology 44 17934511
2002 Cerebellar lesion up-regulates P2X1 and P2X2 purinergic receptors in precerebellar nuclei. Neuroscience 44 12421608
2000 The novel pyridoxal-5'-phosphate derivative PPNDS potently antagonizes activation of P2X(1) receptors. European journal of pharmacology 42 10650184
2014 The P2X1 receptor is required for neutrophil extravasation during lipopolysaccharide-induced lethal endotoxemia in mice. Journal of immunology (Baltimore, Md. : 1950) 41 25480563
2007 Identification of atropine- and P2X1 receptor antagonist-resistant, neurogenic contractions of the urinary bladder. The Journal of neuroscience : the official journal of the Society for Neuroscience 41 17251425
2005 Contribution of conserved polar glutamine, asparagine and threonine residues and glycosylation to agonist action at human P2X1 receptors for ATP. Journal of neurochemistry 41 16371009
2012 Molecular basis of selective antagonism of the P2X1 receptor for ATP by NF449 and suramin: contribution of basic amino acids in the cysteine-rich loop. British journal of pharmacology 40 21671897
2011 Cysteine scanning mutagenesis (residues Glu52-Gly96) of the human P2X1 receptor for ATP: mapping agonist binding and channel gating. The Journal of biological chemistry 40 21690089
2017 P2X1, P2X4, and P2X7 Receptor Knock Out Mice Expose Differential Outcome of Sepsis Induced by α-Haemolysin Producing Escherichia coli. Frontiers in cellular and infection microbiology 39 28428949
1998 The distribution of single P2x1-receptor clusters on smooth muscle cells in relation to nerve varicosities in the rat urinary bladder. Journal of neurocytology 39 11246492
2021 Targeting P2RX1 alleviates renal ischemia/reperfusion injury by preserving mitochondrial dynamics. Pharmacological research 38 34091010
2013 Male contraception via simultaneous knockout of α1A-adrenoceptors and P2X1-purinoceptors in mice. Proceedings of the National Academy of Sciences of the United States of America 38 24297884
2006 P2X1 stimulation promotes thrombin receptor-mediated platelet aggregation. Journal of thrombosis and haemostasis : JTH 38 16634759
2001 Transient expression of P2X(1) receptor subunits of ATP-gated ion channels in the developing rat cochlea. Brain research. Developmental brain research 38 11248351
2010 P2X(1) receptor blockade inhibits whole kidney autoregulation of renal blood flow in vivo. American journal of physiology. Renal physiology 37 20335318
2002 Effects of enhanced P2X1 receptor Ca2+ influx on functional responses in human platelets. Thrombosis and haemostasis 37 12353081
2004 Heterogeneity of P2X receptors in sympathetic neurons: contribution of neuronal P2X1 receptors revealed using knockout mice. Molecular pharmacology 36 14722245
2002 P2X(1) receptor subunit contribution to gating revealed by a dominant negative PKC mutant. Biochemical and biophysical research communications 36 11855833
2008 Direct modulation of P2X1 receptor-channels by the lipid phosphatidylinositol 4,5-bisphosphate. Molecular pharmacology 35 18523136
1998 Identification of a P2X1 purinoceptor expressed on human platelets. Biochemical and biophysical research communications 35 9464249
2000 Antagonism by the suramin analogue NF279 on human P2X(1) and P2X(7) receptors. European journal of pharmacology 34 10650169
2006 Differential sensitivity of human platelet P2X1 and P2Y1 receptors to disruption of lipid rafts. Biochemical and biophysical research communications 32 16546137
1998 Modulation of ATP-gated non-selective cation channel (P2X1 receptor) activation and desensitization by the actin cytoskeleton. The Journal of physiology 32 9625863
2008 The ATP-gated P2X1 receptor plays a pivotal role in activation of aspirin-treated platelets by thrombin and epinephrine. The Journal of biological chemistry 31 18480058
2004 Vanilloid receptor like 1 (VRL1) immunoreactivity in mammalian retina: colocalization with somatostatin and purinergic P2X1 receptors. The Journal of comparative neurology 31 15174083
2012 Platelet Ca(2+) responses coupled to glycoprotein VI and Toll-like receptors persist in the presence of endothelial-derived inhibitors: roles for secondary activation of P2X1 receptors and release from intracellular Ca(2+) stores. Blood 30 22228626
2003 Lack of evidence for functional ADP-activated human P2X1 receptors supports a role for ATP during hemostasis and thrombosis. Blood 30 12907444
2003 Potentiation of platelet activation through the stimulation of P2X1 receptors. Journal of thrombosis and haemostasis : JTH 30 14675100
1999 No requirement of P2X1 purinoceptors for platelet aggregation. European journal of pharmacology 30 10395026
2014 Extracellular ATP induces intracellular alpha-synuclein accumulation via P2X1 receptor-mediated lysosomal dysfunction. Neurobiology of aging 29 25480524
2012 Expression of P2X₁ and P2X₄ receptors in rat trigeminal ganglion neurons. Neuroreport 29 22785548
2008 Ectodomain lysines and suramin block of P2X1 receptors. The Journal of biological chemistry 29 18765669
2017 Physiopathological implications of P2X1 and P2X7 receptors in regulation of glomerular hemodynamics in angiotensin II-induced hypertension. American journal of physiology. Renal physiology 28 28404593
2010 P2X1 receptor mobility and trafficking; regulation by receptor insertion and activation. Journal of neurochemistry 28 20374431
2009 Contribution of the region Glu181 to Val200 of the extracellular loop of the human P2X1 receptor to agonist binding and gating revealed using cysteine scanning mutagenesis. Journal of neurochemistry 28 19519776
2008 Pharmacological characterization of P2X1 and P2X3 purinergic receptors in bovine chondrocytes. Osteoarthritis and cartilage 28 18448363
2003 Pharmacological identification of P2X1, P2X4 and P2X7 nucleotide receptors in the smooth muscles of human umbilical cord and chorionic blood vessels. Placenta 28 12495655
2012 Immunosuppression preserves renal autoregulatory function and microvascular P2X(1) receptor reactivity in ANG II-hypertensive rats. American journal of physiology. Renal physiology 27 23269644
2019 Identification of aurintricarboxylic acid as a potent allosteric antagonist of P2X1 and P2X3 receptors. Neuropharmacology 26 31461640
1996 A comparison of the binding characteristics of recombinant P2X1 and P2X2 purinoceptors. British journal of pharmacology 26 8842447
2012 Heat shock protein 90 inhibitors reduce trafficking of ATP-gated P2X1 receptors and human platelet responsiveness. The Journal of biological chemistry 25 22851178
2014 Comparative analysis of P2X1, P2X2, P2X3, and P2X4 receptor subunits in rat nodose ganglion neurons. PloS one 24 24798490
2009 P2X(1) receptor inhibition and soluble CD39 administration as novel approaches to widen the cardiovascular therapeutic window. Trends in cardiovascular medicine 23 19467446
2000 The purinergic calcium channels P2X1,2,5,7 are down-regulated while P2X3,4,6 are up-regulated during apoptosis in the ageing rat prostate. The Histochemical journal 23 11127979
2014 Ca2+ influx through P2X1 receptors amplifies P2Y1 receptor-evoked Ca2+ signaling and ADP-evoked platelet aggregation. Molecular pharmacology 22 24923466