ArticleBritish journal of pharmacology2008
Novel consequences of voltage-dependence to G-protein-coupled P2Y1 receptors.
Article in British journal of pharmacology, 2008. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
21 citing papers in PubMed, 32 citations in OpenAlex.
- A voltage-dependent switch underlies efficient yet specific learning and memory.Current biology : CB · 2026Article
- Action Potential Firing Patterns Regulate Dopamine Release via Voltage-Sensitive Dopamine D2 Autoreceptors in Mouse Striatum In Vivo.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Charge Movements and Conformational Changes: Biophysical Properties and Physiology of Voltage-Dependent GPCRs.Biomolecules · 2024Review
- Understanding electrical and chemical transmission in the brain.Frontiers in cellular neuroscience · 2024Review
- Article
- GPCR voltage dependence controls neuronal plasticity and behavior.Nature communications · 2021Article
- Regulating quantal size of neurotransmitter release through a GPCR voltage sensor.Proceedings of the National Academy of Sciences of the United States of America · 2020Article
- Voltage modulates the effect of μ-receptor activation in a ligand-dependent manner.British journal of pharmacology · 2020Article
- Membrane potentials regulating GPCRs: insights from experiments and molecular dynamics simulations.Current opinion in pharmacology · 2016Review
- Modeling Interactions among Individual P2 Receptors to Explain Complex Response Patterns over a Wide Range of ATP Concentrations.Frontiers in physiology · 2016Article
- Blood cells: an historical account of the roles of purinergic signalling.Purinergic signalling · 2015Review
- Membrane Potential Controls the Efficacy of Catecholamine-induced β1-Adrenoceptor Activity.The Journal of biological chemistry · 2015Article
- Article
- Novel insights on thyroid-stimulating hormone receptor signal transduction.Endocrine reviews · 2013Review
- Administration of exogenous adenosine triphosphate to ischemic skeletal muscle induces an energy-sparing effect: role of adenosine receptors.The Journal of surgical research · 2013Article
- Voltage regulates adrenergic receptor function.Proceedings of the National Academy of Sciences of the United States of America · 2013Article
- P2Y1 receptor modulation of Ca2+-activated K+ currents in medium-sized neurons from neonatal rat striatal slices.Journal of neurophysiology · 2012Article
- Depolarization induces a conformational change in the binding site region of the M2 muscarinic receptor.Proceedings of the National Academy of Sciences of the United States of America · 2012Article
- Calcium signals in the nucleus accumbens: activation of astrocytes by ATP and succinate.BMC neuroscience · 2011Article
- Direct voltage control of endogenous lysophosphatidic acid G-protein-coupled receptors in Xenopus oocytes.The Journal of physiology · 2010Article
Corrections and comments
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Authors and funding
3 authors at 2 institutions in 2 countries.
Funding
Abstract
background and purposeEmerging evidence suggests that activation of G-protein-coupled receptors (GPCRs) can be directly regulated by membrane voltage. However, the physiological and pharmacological relevance of this effect remains unclear. We have further examined this phenomenon for P2Y1 receptors in the non-excitable megakaryocyte using a range of agonists and antagonists. EXPERIMENTAL APPROACH: Simultaneous whole-cell patch clamp and fura-2 fluorescence recordings of rat megakaryocytes, which lack voltage-gated Ca2+ influx, were used to examine the voltage-dependence of P2Y1 receptor-evoked IP3-dependent Ca2+ mobilization.
resultsDepolarization transiently and repeatedly enhanced P2Y1 receptor-evoked Ca2+ mobilization across a wide concentration range of both weak, partial and full, potent agonists. Moreover, the amplitude of the depolarization-evoked [Ca2+]i increase displayed an inverse relationship with agonist concentration, such that the greatest potentiating effect of voltage was observed at near-threshold levels of agonist. Unexpectedly, depolarization also stimulated an [Ca2+]i increase in the absence of agonist during exposure to the competitive antagonists A3P5PS and MRS2179, or the allosteric enhancer 2,2'-pyridylisatogen tosylate. A further effect of some antagonists, particularly suramin, was to enhance the depolarization-evoked Ca2+ responses during co-application of an agonist. Of several P2Y1 receptor inhibitors, only SCH202676, which has a proposed allosteric mechanism of action, could block ADP-induced voltage-dependent Ca2+ release. CONCLUSIONS AND IMPLICATIONS: The ability of depolarization to potentiate GPCRs at near-threshold agonist concentrations represents a novel mechanism for coincidence detection. Furthermore, the induction and enhancement of voltage-dependent GPCR responses by antagonists has implications for the design of therapeutic compounds.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.