| http://purl.uniprot.org/citations/27576299 | http://www.w3.org/1999/02/22-rdf-syntax-ns#type | http://purl.uniprot.org/core/Journal_Citation |
| http://purl.uniprot.org/citations/27576299 | http://www.w3.org/2000/01/rdf-schema#comment | "Accumulating evidence indicates that purinergic P2X4 receptors (P2X4R: cation channels activated by extracellular ATP) expressed in spinal microglia are crucial for pathological chronic pain caused by nerve damage, suggesting a potential target for drug discovery. We identified NP-1815-PX (5-[3-(5-thioxo-4H-[1,2,4]oxadiazol-3-yl)phenyl]-1H-naphtho[1, 2-b][1,4]diazepine-2,4(3H,5H)-dione) as a novel antagonist selective for P2X4R with high potency and selectivity compared with other P2XR subtypes. In in vivo assay for acute and chronic pain, intrathecal administration of NP-1815-PX produced an anti-allodynic effect in mice with traumatic nerve damage without affecting acute nociceptive pain and motor function (although its oral administration did not produce the effect). Furthermore, in a mouse model of herpetic pain, P2X4R upregulation in the spinal cord exclusively occurred in microglia, and intrathecal NP-1815-PX suppressed induction of mechanical allodynia. This model also showed K(+)/Cl(-) cotransporter 2 (KCC2) downregulation, which is implicated in dorsal horn neuron hyperexcitability; this downregulation was restored by intrathecal treatment with NP-1815-PX or by interfering with brain-derived neurotrophic factor (BDNF) signaling, a P2X4R-activated microglial factor implicated in KCC2 downregulation. Taken together, the newly developed P2X4R antagonist NP-1815-PX produces anti-allodynic effects in chronic pain models without altering acute pain sensitivity, suggesting that microglial P2X4R could be an attractive target for treating chronic pain."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.org/dc/terms/identifier | "doi:10.1038/srep32461"xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Inoue K."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Kohno K."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Imai T."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Masuda T."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Tsuda M."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Sasaki A."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Yamashita T."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Matsumura Y."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Kuraishi Y."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Nakata E."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/author | "Tozaki-Saitoh H."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/date | "2016"xsd:gYear |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/name | "Sci Rep"xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/pages | "32461"xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/title | "A novel P2X4 receptor-selective antagonist produces anti-allodynic effect in a mouse model of herpetic pain."xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://purl.uniprot.org/core/volume | "6"xsd:string |
| http://purl.uniprot.org/citations/27576299 | http://www.w3.org/2004/02/skos/core#exactMatch | http://purl.uniprot.org/pubmed/27576299 |
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