Piperazine squaric acid diamides, a novel class of allosteric P2X7 receptor antagonists

2021 ◽  
pp. 113838
Author(s):  
Marius Patberg ◽  
Andreas Isaak ◽  
Friederike Füsser ◽  
Natalia V. Ortiz Zacarías ◽  
Laura Vinnenberg ◽  
...  
Keyword(s):  
P2x7 Receptor ◽  
Squaric Acid ◽  
Receptor Antagonists

scholarly journals Functional Coupling between the P2X7 Receptor and Pannexin-1 Channel in Rat Trigeminal Ganglion Neurons

2021 ◽  
Vol 22 (11) ◽  
pp. 5978
Author(s):  
Hiroyuki Inoue ◽  
Hidetaka Kuroda ◽  
Wataru Ofusa ◽  
Sadao Oyama ◽  
Maki Kimura ◽  
...  
Keyword(s):  
Trigeminal Ganglion ◽  
P2x7 Receptor ◽  
P2x Receptor ◽  
Functional Coupling ◽  
Dependent Manner ◽  
High Concentration ◽  
Receptor Antagonists ◽  
P2x7 Receptors ◽  
Pannexin 1 ◽  
Ganglion Neurons

The ionotropic P2X receptor, P2X7, is believed to regulate and/or generate nociceptive pain, and pain in several neuropathological diseases. Although there is a known relationship between P2X7 receptor activity and pain sensing, its detailed functional properties in trigeminal ganglion (TG) neurons remains unclear. We examined the electrophysiological and pharmacological characteristics of the P2X7 receptor and its functional coupling with other P2X receptors and pannexin-1 (PANX1) channels in primary cultured rat TG neurons, using whole-cell patch-clamp recordings. Application of ATP and Bz-ATP induced long-lasting biphasic inward currents that were more sensitive to extracellular Bz-ATP than ATP, indicating that the current was carried by P2X7 receptors. While the biphasic current densities of the first and second components were increased by Bz-ATP in a concentration dependent manner; current duration was only affected in the second component. These currents were significantly inhibited by P2X7 receptor antagonists, while only the second component was inhibited by P2X1, 3, and 4 receptor antagonists, PANX1 channel inhibitors, and extracellular ATPase. Taken together, our data suggests that autocrine or paracrine signaling via the P2X7-PANX1-P2X receptor/channel complex may play important roles in several pain sensing pathways via long-lasting neuronal activity driven by extracellular high-concentration ATP following tissue damage in the orofacial area.

Novel Series of Dihydropyridinone P2X7 Receptor Antagonists

2015 ◽  
Vol 58 (21) ◽  
pp. 8413-8426 ◽  
Author(s):  
Francisco Lopez-Tapia ◽  
Keith A. M. Walker ◽  
Christine Brotherton-Pleiss ◽  
Joanie Caroon ◽  
Dov Nitzan ◽  
...  
Keyword(s):  
P2x7 Receptor ◽  
Receptor Antagonists

Synthesis and structure-activity relationships of quinolinone and quinoline-based P2X7 receptor antagonists and their anti-sphere formation activities in glioblastoma cells

2018 ◽  
Vol 151 ◽  
pp. 462-481 ◽  
Author(s):  
Seung-Hwa Kwak ◽  
Seungheon Shin ◽  
Ji-Hyun Lee ◽  
Jin-Kyoung Shim ◽  
Minjeong Kim ◽  
...  
Keyword(s):  
P2x7 Receptor ◽  
Glioblastoma Cells ◽  
Receptor Antagonists ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Sphere Formation

Abstract 2582: P2X7 receptor is functional in myeloma cell lines and myeloma patient cells and can be modulated by P2X7 receptor antagonists: Implications for myeloma therapy

2011 ◽  
Author(s):  
Kathleen A. Donovan ◽  
Laurie Moon-Tasson ◽  
Alexander E. Hromockyj ◽  
Debra M. Meyer ◽  
John A. Lust
Keyword(s):  
Cell Lines ◽  
P2x7 Receptor ◽  
Myeloma Cell ◽  
Myeloma Patient ◽  
Receptor Antagonists

scholarly journals Novel P2X7 receptor antagonists ease the pain

2007 ◽  
Vol 151 (5) ◽  
pp. 565-567 ◽  
Author(s):  
B F King
Keyword(s):  
P2x7 Receptor ◽  
Receptor Antagonists

Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3- a ]pyrazin-8(5 H )-one P2X7 receptor antagonists

2016 ◽  
Vol 26 (2) ◽  
pp. 257-261 ◽  
Author(s):  
Michael K. Ameriks ◽  
Hong Ao ◽  
Nicholas I. Carruthers ◽  
Brian Lord ◽  
Suchitra Ravula ◽  
...  
Keyword(s):  
P2x7 Receptor ◽  
Receptor Antagonists

Purinergic P2X7 receptor antagonists: Chemistry and fundamentals of biological screening

2009 ◽  
Vol 17 (14) ◽  
pp. 4861-4865 ◽  
Author(s):  
Hendra Gunosewoyo ◽  
Mark J. Coster ◽  
Maxwell R. Bennett ◽  
Michael Kassiou
Keyword(s):  
P2x7 Receptor ◽  
Receptor Antagonists ◽  
Biological Screening ◽  
Purinergic P2x7 Receptor

Effects of P2X7 receptor antagonists on hypoxia-induced neonatal seizures in mice

2017 ◽  
Vol 116 ◽  
pp. 351-363 ◽  
Author(s):  
Natalia Rodriguez-Alvarez ◽  
Eva M. Jimenez-Mateos ◽  
Tobias Engel ◽  
Sean Quinlan ◽  
Cristina R. Reschke ◽  
...  
Keyword(s):  
P2x7 Receptor ◽  
Neonatal Seizures ◽  
Receptor Antagonists

scholarly journals Mechanism of action of species-selective P2X7 receptor antagonists

2009 ◽  
Vol 156 (8) ◽  
pp. 1312-1325 ◽  
Author(s):  
Anton D Michel ◽  
Sin-Wei Ng ◽  
Shilina Roman ◽  
William C Clay ◽  
David K Dean ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
P2x7 Receptor ◽  
Receptor Antagonists

Synthesis and SAR development of novel P2X7 receptor antagonists for the treatment of pain: Part 2

2011 ◽  
Vol 21 (24) ◽  
pp. 7287-7290 ◽  
Author(s):  
Stephanie Brumfield ◽  
Julius J. Matasi ◽  
Deen Tulshian ◽  
Michael Czarniecki ◽  
William Greenlee ◽  
...  
Keyword(s):  
P2x7 Receptor ◽  
Receptor Antagonists
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