| pubmed-article:15685199 | rdf:type | pubmed:Citation | lld:pubmed |
| pubmed-article:15685199 | lifeskim:mentions | umls-concept:C0086418 | lld:lifeskim |
| pubmed-article:15685199 | lifeskim:mentions | umls-concept:C0025936 | lld:lifeskim |
| pubmed-article:15685199 | lifeskim:mentions | umls-concept:C0597357 | lld:lifeskim |
| pubmed-article:15685199 | lifeskim:mentions | umls-concept:C0384601 | lld:lifeskim |
| pubmed-article:15685199 | lifeskim:mentions | umls-concept:C0441655 | lld:lifeskim |
| pubmed-article:15685199 | lifeskim:mentions | umls-concept:C0231491 | lld:lifeskim |
| pubmed-article:15685199 | lifeskim:mentions | umls-concept:C0679622 | lld:lifeskim |
| pubmed-article:15685199 | lifeskim:mentions | umls-concept:C0205314 | lld:lifeskim |
| pubmed-article:15685199 | pubmed:issue | 7 | lld:pubmed |
| pubmed-article:15685199 | pubmed:dateCreated | 2005-4-4 | lld:pubmed |
| pubmed-article:15685199 | pubmed:abstractText | We describe the properties of a novel nonpeptide kinin B1 receptor antagonist, NVP-SAA164, and demonstrate its in vivo activity in models of inflammatory pain in transgenic mice expressing the human B1 receptor. NVP-SAA164 showed high affinity for the human B1 receptor expressed in HEK293 cells (K(i) 8 nM), and inhibited increases in intracellular calcium induced by desArg10kallidin (desArg10KD) (IC50 33 nM). While a similar high affinity was observed in monkey fibroblasts (K(i) 7.7 nM), NVP-SAA164 showed no affinity for the rat B1 receptor expressed in Cos-7 cells. In transgenic mice in which the native B1 receptor was deleted and the gene encoding the human B1 receptor was inserted (hB1 knockin, hB1-KI), hB1 receptor mRNA was induced in tissues following LPS treatment. No mRNA encoding the mouse or human B1 receptor was detected in mouse B1 receptor knockout (mB1-KO) mice following LPS treatment. Freund's complete adjuvant-induced mechanical hyperalgesia was similar in wild-type and hB(1)-KI mice, but was significantly reduced in mB1-KO animals. Mechanical hyperalgesia induced by injection of the B1 agonist desArg10KD into the contralateral paw 24 h following FCA injection was similar in wild-type and hB1-KI mice, but was absent in mB1-KO animals. Oral administration of NVP-SAA164 produced a dose-related reversal of FCA-induced mechanical hyperalgesia and desArg10KD-induced hyperalgesia in hB1-KI mice, but was inactive against inflammatory pain in wild-type mice. These data demonstrate the use of transgenic technology to investigate the in vivo efficacy of species selective agents and show that NVP-SAA164 is a novel orally active B1 receptor antagonist, providing further support for the utility of B1 receptor antagonists in inflammatory pain conditions in man. | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:commentsCorrections | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:language | eng | lld:pubmed |
| pubmed-article:15685199 | pubmed:journal | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:citationSubset | IM | lld:pubmed |
| pubmed-article:15685199 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:chemical | http://linkedlifedata.com/r... | lld:pubmed |
| pubmed-article:15685199 | pubmed:status | MEDLINE | lld:pubmed |
| pubmed-article:15685199 | pubmed:month | Apr | lld:pubmed |
| pubmed-article:15685199 | pubmed:issn | 0007-1188 | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:ShumP SPS | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:BevanStuartS | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:DragoniIlaria... | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:McIntyrePeter... | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:FoxAlysonA | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:DavisClareC | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:ColleySianS | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:BurgessGillia... | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:KaurSatbirS | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:LiBifangB | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:PanesarMohM | lld:pubmed |
| pubmed-article:15685199 | pubmed:author | pubmed-author:RitchieTimT | lld:pubmed |
| pubmed-article:15685199 | pubmed:issnType | Print | lld:pubmed |
| pubmed-article:15685199 | pubmed:volume | 144 | lld:pubmed |
| pubmed-article:15685199 | pubmed:owner | NLM | lld:pubmed |
| pubmed-article:15685199 | pubmed:authorsComplete | Y | lld:pubmed |
| pubmed-article:15685199 | pubmed:pagination | 889-99 | lld:pubmed |
| pubmed-article:15685199 | pubmed:dateRevised | 2009-11-18 | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:meshHeading | pubmed-meshheading:15685199... | lld:pubmed |
| pubmed-article:15685199 | pubmed:year | 2005 | lld:pubmed |
| pubmed-article:15685199 | pubmed:articleTitle | Antihyperalgesic activity of a novel nonpeptide bradykinin B1 receptor antagonist in transgenic mice expressing the human B1 receptor. | lld:pubmed |
| pubmed-article:15685199 | pubmed:affiliation | Novartis Institutes for Biomedical Research, 5 Gower Place, London WC1E 6BS. alyson.fox@pharma.novartis.com | lld:pubmed |
