| pubmed-article:12482951 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0034721 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0034693 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0027796 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0597357 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C1423503 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0333348 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C1418212 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0392756 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0205191 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:12482951 | lifeskim:mentions | umls-concept:C1449407 | lld:lifeskim |
| pubmed-article:12482951 | pubmed:issue | 26 | lld:pubmed |
| pubmed-article:12482951 | pubmed:dateCreated | 2002-12-24 | lld:pubmed |
| pubmed-article:12482951 | pubmed:abstractText | P2X3 and P2X2/3 receptors are highly localized on peripheral and central processes of sensory afferent nerves, and activation of these channels contributes to the pronociceptive effects of ATP. A-317491 is a novel non-nucleotide antagonist of P2X3 and P2X2/3 receptor activation. A-317491 potently blocked recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and was highly selective (IC50 >10 microM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 also blocked native P2X3 and P2X2/3 receptors in rat dorsal root ganglion neurons. Blockade of P2X3 containing channels was stereospecific because the R-enantiomer (A-317344) of A-317491 was significantly less active at P2X3 and P2X2/3 receptors. A-317491 dose-dependently (ED50 = 30 micromolkg s.c.) reduced complete Freund's adjuvant-induced thermal hyperalgesia in the rat. A-317491 was most potent (ED50 = 10-15 micromolkg s.c.) in attenuating both thermal hyperalgesia and mechanical allodynia after chronic nerve constriction injury. The R-enantiomer, A-317344, was inactive in these chronic pain models. Although active in chronic pain models, A-317491 was ineffective (ED50 >100 micromolkg s.c.) in reducing nociception in animal models of acute pain, postoperative pain, and visceral pain. The present data indicate that a potent and selective antagonist of P2X3 and P2X2/3 receptors effectively reduces both nerve injury and chronic inflammatory nociception, but P2X3 and P2X2/3 receptor activation may not be a major mediator of acute, acute inflammatory, or visceral pain. | lld:pubmed |
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| pubmed-article:12482951 | pubmed:language | eng | lld:pubmed |
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| pubmed-article:12482951 | pubmed:citationSubset | IM | lld:pubmed |
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| pubmed-article:12482951 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:12482951 | pubmed:month | Dec | lld:pubmed |
| pubmed-article:12482951 | pubmed:issn | 0027-8424 | lld:pubmed |
| pubmed-article:12482951 | pubmed:author | pubmed-author:CoxBryan FBF | lld:pubmed |
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| pubmed-article:12482951 | pubmed:author | pubmed-author:FaltynekConni... | lld:pubmed |
| pubmed-article:12482951 | pubmed:author | pubmed-author:CartmellJayne... | lld:pubmed |
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| pubmed-article:12482951 | pubmed:author | pubmed-author:BrennanTimoth... | lld:pubmed |
| pubmed-article:12482951 | pubmed:author | pubmed-author:BianchiBruceB | lld:pubmed |
| pubmed-article:12482951 | pubmed:author | pubmed-author:YuHaixiaH | lld:pubmed |
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| pubmed-article:12482951 | pubmed:author | pubmed-author:ChuKatharineK | lld:pubmed |
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| pubmed-article:12482951 | pubmed:author | pubmed-author:LynchKevinK | lld:pubmed |
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| pubmed-article:12482951 | pubmed:author | pubmed-author:KageKarenK | lld:pubmed |
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| pubmed-article:12482951 | pubmed:author | pubmed-author:ZhuChang ZCZ | lld:pubmed |
| pubmed-article:12482951 | pubmed:author | pubmed-author:Van... | lld:pubmed |
| pubmed-article:12482951 | pubmed:author | pubmed-author:KowalukElizab... | lld:pubmed |
| pubmed-article:12482951 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:12482951 | pubmed:day | 24 | lld:pubmed |
| pubmed-article:12482951 | pubmed:volume | 99 | lld:pubmed |
| pubmed-article:12482951 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:12482951 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:12482951 | pubmed:pagination | 17179-84 | lld:pubmed |
| pubmed-article:12482951 | pubmed:dateRevised | 2010-11-18 | lld:pubmed |
| pubmed-article:12482951 | pubmed:meshHeading | pubmed-meshheading:12482951... | lld:pubmed |
| pubmed-article:12482951 | pubmed:meshHeading | pubmed-meshheading:12482951... | lld:pubmed |
