ArticleThe Journal of physiology2001
Functional evidence of distinct ATP activation sites at the human P2X(7) receptor.
Article in The Journal of physiology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 75 citations in OpenAlex.
- A brain-penetrant P2X7R antagonist mitigates Alzheimer's disease pathology.bioRxiv : the preprint server for biology · 2026Article
- Generalised Hodgkin-Huxley model captures human P2X and AMPA receptor currents.The Journal of physiology · 2026Article
- A polycyclic scaffold identified by structure-based drug design effectively inhibits the human P2X7 receptor.Nature communications · 2025Article
- Article
- Two serial filters control P2X7 cation selectivity, Ser342 in the central pore and lateral acidic residues at the cytoplasmic interface.PNAS nexus · 2024Article
- The Pannexin 1 Channel and the P2X7 Receptor Are in Complex Interplay to Regulate the Release of Soluble Ectonucleotidases in the Murine Bladder Lamina Propria.International journal of molecular sciences · 2023Article
- Rehabilitation of the P2X5 receptor: a re-evaluation of structure and function.Purinergic signalling · 2023Review
- Article
- Dihydropyridines Potentiate ATP-Induced Currents Mediated by the Full-Length Human P2X5 Receptor.Molecules (Basel, Switzerland) · 2022Article
- Mathematical modelling of human P2X-mediated plasma membrane electrophysiology and calcium dynamics in microglia.PLoS computational biology · 2021Article
- Dissection of P2X4 and P2X7 Receptor Current Components in BV-2 Microglia.International journal of molecular sciences · 2020Article
- Amyloid Beta Peptide (AβJournal of clinical medicine · 2020Article
- β-Nicotinamide Adenine Dinucleotide (β-NAD) Inhibits ATP-Dependent IL-1β Release from Human Monocytic Cells.International journal of molecular sciences · 2018Article
- Methylene blue relieves the development of osteoarthritis by upregulating lncRNA MEG3.Experimental and therapeutic medicine · 2018Article
- Article
- Interaction of Purinergic P2X4 and P2X7 Receptor Subunits.Frontiers in pharmacology · 2017Article
- Homodimeric anoctamin-1, but not homodimeric anoctamin-6, is activated by calcium increases mediated by the P2Y1 and P2X7 receptors.Pflugers Archiv : European journal of physiology · 2015Article
- Allosteric regulation of the P2X4 receptor channel pore dilation.Pflugers Archiv : European journal of physiology · 2015Article
- Rat submandibular glands secrete nanovesicles with NTPDase and 5'-nucleotidase activities.Purinergic signalling · 2015Article
- Regulation of ATP-gated P2X channels: from redox signaling to interactions with other proteins.Antioxidants & redox signaling · 2014Review
Corrections and comments
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Authors and funding
4 authors at 2 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The effect of the agonist ATP on whole cell currents of Xenopus oocytes expressing either the wild-type human P2X(7) receptor (hP2X(7)), an N-terminally hexahistidyl-tagged hP2X(7) receptor (His-hP2X(7)), or a truncated His-hP2X(7) receptor (His-hP2X(7)DeltaC) lacking the C-terminal 156 amino acids was investigated using the two-microelectrode voltage clamp technique. 2. The activation time course of the wild-type hP2X(7) receptor can be described as the sum of an exponentially growing and an additional almost linearly activating current component. 3. The amplitude of the exponentially activating current component of the wild-type hP2X(7) receptor displayed a biphasic dependence on the agonist concentration, which could be best approximated by a model of two equal high-sensitivity and two equal low-sensitivity non-cooperative activation sites with apparent dissociation constants of about 4 and 200 microM free ATP(4-), respectively. 4. The linearly activating current was monophasically dependent on the agonist concentration with an apparent dissociation constant of about 200 microM. 5. The contribution of the low-sensitivity sites to current kinetics was reduced or almost abolished in oocytes expressing His-hP2X(7) or His-hP2X(7)DeltaC. 6. Our data indicate that the hP2X(7) receptor possesses at least two types of activation sites, which differ in ATP(4-) sensitivity by a factor of 50. The degree of occupation of these two sites influences both activation and deactivation kinetics. Both N- and C-terminal domains appear to be important determinants of the current elicited by activation of the sites with low ATP sensitivity, but not for that mediated by the highly ATP-sensitive sites.
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