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Structure-activity relationship studies on a series of novel, substituted 1-benzyl-5-phenyltetrazole P2X7 antagonists.
1-Benzyl-5-aryltetrazoles were discovered to be novel antagonists for the P2X(7) receptor and advanced to efficacy studies in a model of neuropathic pain where significant reversal of mechanical allodynia was observed at doses that did not affect motor coordination.
A-317491, a novel potent and selective non-nucleotide antagonist of P2X3 and P2X2/3 receptors, reduces chronic inflammatory and neuropathic pain in the rat
The present data indicate that a potent and selective antagonist of P 2X3 and P2X2/3 receptors effectively reduces both nerve injury and chronic inflammatory nociception, but P2x3 andP2X 2/3 receptor activation may not be a major mediator of acute, acute inflammatory, or visceral pain.
A-740003 [N-(1-{[(Cyanoimino)(5-quinolinylamino) methyl]amino}-2,2-dimethylpropyl)-2-(3,4-dimethoxyphenyl)acetamide], a Novel and Selective P2X7 Receptor Antagonist, Dose-Dependently Reduces
It is demonstrated that selective blockade of P2X7 receptors in vivo produces significant antinociception in animal models of neuropathic and inflammatory pain.
Pharmacological characterization of recombinant human and rat P2X receptor subtypes.
ATP-gated P2X cation-channels
A summary of the pharmacology of recombinant homomeric and heteromeric P2X receptors, with particular emphasis on new antagonists, is presented.
A-803467, a potent and selective Nav1.8 sodium channel blocker, attenuates neuropathic and inflammatory pain in the rat
A-803467 is found, a sodium channel blocker that potently blocks tetrodotoxin-resistant currents and the generation of spontaneous and electrically evoked action potentials in vitro in rat dorsal root ganglion neurons and produces significant antinociception in animal models of neuropathic and inflammatory pain.
Purine and pyrimidine (P2) receptors as drug targets.
Mammalian P2X7 receptor pharmacology: comparison of recombinant mouse, rat and human P2X7 receptors
Acute activation of P2X7 receptors rapidly opens a non‐selective cation channel and sustained P2x7 receptor activation leads to the formation of cytolytic pores, mediated by downstream recruitment of hemichannels to the cell surface.
Discovery of P2X7 receptor‐selective antagonists offers new insights into P2X7 receptor function and indicates a role in chronic pain states
This review incorporates the recent discoveries of novel P2X7 receptor‐selective antagonists with a brief update on P2 X7 receptor pharmacology and its therapeutic potential and offers new evidence that P2x7 receptors play a specific role in nociceptive signaling in chronic pain states.