P2X3 receptor
Extracellular ATP-gated cation channel (purinoceptor)
(Alternative nomenclature: purinergic receptor P2X3, P2X3R)
P2X3 is an extracellular ATP-gated cation channel that mediates currents in sensory neurons. Activation by ATP causes depolarization. Important for nociception. Each subunit has 2-TM. Functional channels are tri- or tetramers.
Localization:
Sensory neurons. Main P2X receptor in small dorsal root ganglion cells, trigeminal ganglion, central projections (inner lamina II of spinal dorsal horn), solitary nucleus, tubular viscera
Information links:
http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=600843
QPatch recording of P2X3 receptor currents:.jpg)
P2X3 current sweeps from αβ-methyl ATP dose-response experiment. The green bar represents the position of the user defined cursor for current amplitude measurements.
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Hill fit and EC50 determination of αβ-methyl ATP for P2X3 receptors. 1 µM agonist was added twice to show the reproduceability of the data.
Pharmacological profiling:
Antagonists:
Agonists:
(The list is not intended to be complete)
Pathophysiology: N/A
Recent review articles:
North RA. P2X3 receptors and peripheral pain mechanisms. J Physiol.,554:301-8, 2005.
Jarvis MF. Contributions of P2X3 homomeric and heteromeric channels to acute and chronic pain.
Expert Opin Ther Targets., 7:513-22, 2003.
QPatch written material:
Application reports:
Characterization of P2X3 receptors by QPatch 16 (293 kB)
P2X3 in CHO Cells
Posters:HTS Screening of hERG Blockers Using 2nd-Generatation Automated Patch-Clamp System, Japanese Pharmacologial Meeting 2005 (1,8 MB)
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