purinergic p2x receptor antagonists


Summary: Compounds that bind to and block the stimulation of PURINERGIC P2X RECEPTORS. Included under this heading are antagonists for specific P2X receptor subtypes.

Top Publications

  1. Rosenthal A, Gohr C, Mitton Fitzgerald E, Lutz M, Dubyak G, Ryan L. The progressive ankylosis gene product ANK regulates extracellular ATP levels in primary articular chondrocytes. Arthritis Res Ther. 2013;15:R154 pubmed publisher
    ..These findings implicate ANK and P2X7/4 receptors in chondrocyte eATP efflux. Understanding the mechanisms of eATP efflux may result in novel therapies for calcium crystal arthritis and osteoarthritis. ..
  2. Platania C, Giurdanella G, Di Paola L, Leggio G, Drago F, Salomone S, et al. P2X7 receptor antagonism: Implications in diabetic retinopathy. Biochem Pharmacol. 2017;138:130-139 pubmed publisher
  3. Hao M, Bergner A, Hirst C, Stamp L, Casagranda F, Bornstein J, et al. Spontaneous calcium waves in the developing enteric nervous system. Dev Biol. 2017;428:74-87 pubmed publisher
    ..One previous study has shown that calcium signalling plays a role in sympathetic ganglia formation; our results suggest that calcium waves are likely to be important for enteric ganglia development. ..
  4. Yoshida K, Ito M, Hoshino Y, Matsuoka I. Effects of dexamethasone on purinergic signaling in murine mast cells: Selective suppression of P2X7 receptor expression. Biochem Biophys Res Commun. 2017;493:1587-1593 pubmed publisher
    ..These results suggest that reduction of P2X7 receptor expression in mast cells might be one of the anti-allergic mechanisms of Dex...
  5. Chen S, Qin T, Seidel J, Zheng Y, Eikermann M, Ferrari M, et al. Inhibition of the P2X7-PANX1 complex suppresses spreading depolarization and neuroinflammation. Brain. 2017;140:1643-1656 pubmed publisher
  6. McLarnon J. Roles of purinergic P2X7 receptor in glioma and microglia in brain tumors. Cancer Lett. 2017;402:93-99 pubmed publisher
    ..Overall, P2X7R activation is associated with a complexity of modulatory actions on tumor growth in part due to ubiquitous expression of the receptor in glioma and immune responsive cells. ..
  7. Ishchenko Y, Novosolova N, Khafizov K, Bart G, Timonina A, Fayuk D, et al. Reconstructed Serine 288 in the Left Flipper Region of the Rat P2X7 Receptor Stabilizes Nonsensitized States. Biochemistry. 2017;56:3394-3402 pubmed publisher
    ..Our combined experimental, kinetic, and molecular modeling data suggest that the rat F288S novel phenotype is due to a slower rate of ATP binding and/or unbinding and stabilization of nonsensitized receptor states. ..
  8. Qi D, Yang Y, Ji P, Kong J, Wu Q, Si H. Upregulation of the Purinergic Receptor Subtype P2X3 in the Trigeminal Ganglion Is Involved in Orofacial Pain Induced by Occlusal Interference in Rats. J Oral Facial Pain Headache. 2016;30:51-60 pubmed publisher
    ..Upregulated P2X3R expression in the TG may contribute to orofacial pain development induced by an occlusal interference. P2X3R may be a therapeutic target for chronic TMJ or masseter muscle pain. ..
  9. Lu W, Albalawi F, Beckel J, Lim J, Laties A, Mitchell C. The P2X7 receptor links mechanical strain to cytokine IL-6 up-regulation and release in neurons and astrocytes. J Neurochem. 2017;141:436-448 pubmed publisher
    ..The mechanosensitive up-regulation and release of cytokine IL-6 from the retina involves the P2X7 receptor, with both astrocytes and neurons contributing to the response. ..

More Information


  1. Geraghty N, Belfiore L, Ly D, Adhikary S, Fuller S, Varikatt W, et al. The P2X7 receptor antagonist Brilliant Blue G reduces serum human interferon-? in a humanized mouse model of graft-versus-host disease. Clin Exp Immunol. 2017;190:79-95 pubmed publisher
    ..In conclusion, the P2X7 antagonist BBG reduced circulating IFN-? in a humanized mouse model of GVHD supporting a potential role for P2X7 to alter the pathology of this disease in humans. ..
  2. Khalafalla M, Woods L, Camden J, Khan A, Limesand K, Petris M, et al. P2X7 receptor antagonism prevents IL-1? release from salivary epithelial cells and reduces inflammation in a mouse model of autoimmune exocrinopathy. J Biol Chem. 2017;292:16626-16637 pubmed publisher
    ..These findings demonstrate that P2X7R antagonism in vivo represents a promising therapeutic strategy to limit salivary gland inflammation and improve secretory function. ..
  3. Letavic M, Savall B, Allison B, Aluisio L, Andrés J, De Angelis M, et al. 4-Methyl-6,7-dihydro-4H-triazolo[4,5-c]pyridine-Based P2X7 Receptor Antagonists: Optimization of Pharmacokinetic Properties Leading to the Identification of a Clinical Candidate. J Med Chem. 2017;60:4559-4572 pubmed publisher
    ..The drug discovery efforts and strategies that resulted in the identification of the clinical candidate are described herein. ..