ArticleNeurobiology of disease2014
Central P2Y12 receptor blockade alleviates inflammatory and neuropathic pain and cytokine production in rodents.
Article in Neurobiology of disease, 2014. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 42 papers, 1 of them a synthesis that pooled it.
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Who cites it
42 citing papers in PubMed, 1 synthesis or guideline pooled it, 88 citations in OpenAlex.
- The efficacy and mechanisms of low-intensity transcranial ultrasound stimulation on pain: a systematic review of human and animal studies.The journal of headache and pain · 2025Pooled it
- Efficacy and Safety of Dorsal Root Ganglion Pulse Radiofrequency Combined With Sympathetic Radiofrequency Ablation in the Treatment of Acute Herpetic Neuralgia.The Clinical journal of pain · 2026Trial
- Clopidogrel, an ADP-P2Y12 Receptor Antagonist, Is Associated With Lower Opioid Consumption and a Reduced Incidence of Delirium in Cancer Patients Receiving Chemotherapy: A Nationwide Retrospective Cohort Study in Japan.Neuropsychopharmacology reports · 2026Article
- Blocking microglial reactivity via purinergic receptors prevents subacute cognitive deficits after TIA.EMBO molecular medicine · 2026Article
- Physical Exercise Improves the Neuronal Function in Ischemic Stroke Via Microglial CBMolecular neurobiology · 2025Article
- The Role of Alpha-7 Nicotinic Acetylcholine Receptors in Pain: Potential Therapeutic Implications.Current neuropharmacology · 2025Review
- Pharmacological interaction and immune response of purinergic receptors in therapeutic modulation.Purinergic signalling · 2024Review
- Electroacupuncture Alleviates Pain by Suppressing P2Y12R-Dependent Microglial Activation in Monoarthritic Rats.Neurochemical research · 2024Article
- Pharmacological characterization of P2Y receptor subtypes - an update.Purinergic signalling · 2024Review
- Blood oxygen regulation via P2Y12R expressed in the carotid body.Respiratory research · 2024Article
- Bone marrow-derived mesenchymal stem cells attenuate complete Freund's adjuvant-induced inflammatory pain by inhibiting the expression of P2X3.Cell proliferation · 2023Article
- Galectin-3 activates spinal microglia to induce inflammatory nociception in wild type but not in mice modelling Alzheimer's disease.Nature communications · 2023Article
- Spinal microglia contribute to sustained inflammatory pain via amplifying neuronal activity.Molecular brain · 2022Article
- A cAMP-Related Gene Network in Microglia Is Inversely Regulated by Morphine Tolerance and Withdrawal.Biological psychiatry global open science · 2022Article
- Exploring the Therapeutic Potential of Targeting Purinergic and Orexinergic Receptors in Alcoholic Neuropathy.Neurotoxicity research · 2022Review
- The Role of Microglial Purinergic Receptors in Pain Signaling.Molecules (Basel, Switzerland) · 2022Review
- Study of the Involvement of the P2Y12 Receptor in Chronic Itching in Type 2 Diabetes Mellitus.Molecular neurobiology · 2022Article
- Selenium-Enriched Yeast Relieves Hexavalent Chromium Toxicity by Inhibiting NF-κB Signaling Pathway in Broiler Spleens.Animals : an open access journal from MDPI · 2022Article
- P2Y12 receptor as a new target for electroacupuncture relieving comorbidity of visceral pain and depression of inflammatory bowel disease.Chinese medicine · 2021Article
- Cangrelor ameliorates CLP-induced pulmonary injury in sepsis by inhibiting GPR17.European journal of medical research · 2021Article
Corrections and comments
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Authors and funding
14 authors at 4 institutions in 2 countries.
Funding
Abstract
In this study the role of P2Y12 receptors (P2Y12R) was explored in rodent models of inflammatory and neuropathic pain and in acute thermal nociception. In correlation with their activity to block the recombinant human P2Y12R, the majority of P2Y12R antagonists alleviated mechanical hyperalgesia dose-dependently, following intraplantar CFA injection, and after partial ligation of the sciatic nerve in rats. They also caused an increase in thermal nociceptive threshold in the hot plate test. Among the six P2Y12R antagonists evaluated in the pain studies, the selective P2Y12 receptor antagonist PSB-0739 was most potent upon intrathecal application. P2Y12R mRNA and IL-1β protein were time-dependently overexpressed in the rat hind paw and lumbar spinal cord following intraplantar CFA injection. This was accompanied by the upregulation of TNF-α, IL-6 and IL-10 in the hind paw. PSB-0739 (0.3mg/kg i.t.) attenuated CFA-induced expression of cytokines in the hind paw and of IL-1β in the spinal cord. Subdiaphragmatic vagotomy and the α7 nicotinic acetylcholine receptor antagonist MLA occluded the effect of PSB-0739 (i.t.) on pain behavior and peripheral cytokine induction. Denervation of sympathetic nerves by 6-OHDA pretreatment did not affect the action of PSB-0739. PSB-0739, in an analgesic dose, did not influence motor coordination and platelet aggregation. Genetic deletion of the P2Y12R in mice reproduced the effect of P2Y12R antagonists on mechanical hyperalgesia in inflammatory and neuropathic pain models, on acute thermal nociception and on the induction of spinal IL-1β. Here we report the robust involvement of the P2Y12R in inflammatory pain. The anti-hyperalgesic effect of P2Y12R antagonism could be mediated by the inhibition of both central and peripheral cytokine production and involves α7-receptor mediated efferent pathways.
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Registered trials
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