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• W2048562538 abstract "Heteromeric P2X2/3 receptors are much more sensitive than homomeric P2X2 receptors to αβ-methylene-ATP, and this ATP analogue is widely used to discriminate the two receptors on sensory neurons and other cells. We sought to determine the structural basis for this selectivity by synthesising ADP and ATP analogues in which the αβ and/or βγ oxygen atoms were replaced by other moieties (including –CH2–, –CHF–, –CHCl–, –CHBr–, –CF2–, –CCl2–, –CBr2–, –CHSO3–, –CHPO3–, –CFPO3–, –CClPO3–, –CH2–CH2–, –C≡C–, –NH–, –CHCOOH–). We tested their actions as agonists or antagonists by whole-cell recording from human embryonic kidney cells expressing P2X2 subunits alone (homomeric P2X2 receptors), or cells expressing both P2X2 and P2X3 subunits, in which the current through heteromeric P2X2/3 receptors was isolated. ADP analogues had no agonist or antagonist effect at either P2X2 or P2X2/3 receptors. All the ATP analogues tested were without agonist or antagonist activity at homomeric P2X2 receptors, except βγ-difluoromethylene-ATP, which was a weak agonist. At P2X2/3 receptors, βγ-imido-ATP, βγ-methylene-ATP, and βγ-acetylene-ATP were weak agonists, whereas αβ,βγ- and βγ,γδ-bismethylene-AP4 were potent full agonists. βγ-Carboxymethylene-ATP and βγ-chlorophosphonomethylene-ATP were weak antagonists at P2X2/3 receptors (IC50 about 10 μM). The results indicate (a) that the homomeric P2X2 receptor presents very stringent structural requirements with respect to its activation by ATP; (b) that the heteromeric P2X2/3 receptor is much more tolerant of αβ and βγ substitution; and (c) that a P2X2/3-selective antagonist can be obtained by introduction of additional negativity at the βγ-methylene. British Journal of Pharmacology (2003) 140, 1027–1034. doi:10.1038/sj.bjp.0705531" @default.
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• W2048562538 date "2003-11-01" @default.
• W2048562538 modified "2023-10-18" @default.
• W2048562538 title "ATP analogues with modified phosphate chains and their selectivity for rat P2X₂ and P2X_2/3 receptors" @default.
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• W2048562538 doi "https://doi.org/10.1038/sj.bjp.0705531" @default.
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