Matches in SemOpenAlex for { <https://semopenalex.org/work/W2110196989> ?p ?o ?g. }
- W2110196989 endingPage "1256" @default.
- W2110196989 startingPage "1248" @default.
- W2110196989 abstract "Indomethacin has been suggested for the treatment of Alzheimer's disease (AD), but its use is limited by gastrointestinal and renal toxicity. To overcome this limitation, D-Pharm Ltd. (Rehovot, Israel) developed DP-155 (mixture of 1-steroyl and 1-palmitoyl-2-{6-[1-(p-chlorobenzoyl)-5-methoxy-2-methyl-3-indolyl acetamido] hexanoyl}-Sn-glycero-3-phosophatidyl [corrected] choline), a lecithin derivative of indomethacin. Safety was tested by daily oral administration of DP-155 or indomethacin to rats in a dose range of 0.007 to 0.28 mmol/kg. The prevalence of gastrointestinal ulceration was significantly lower (10-fold) for DP-155 than for indomethacin, and the ulcerations were delayed. Signs of renal toxicity, namely reduced urine output and increased urine N-acetyl glycosaminidase to creatinine ratio, were 5-fold lower for DP-155. Indomethacin, but not an equimolar dose of DP-155, reduced urine bicyclo-prostaglandin E(2). An equimolar oral dose of DP-155 or indomethacin, administered every 4 h for 3 days, was equally efficacious in reducing the levels of Abeta42 in the brains of Tg2576 mice. Indomethacin was the principal metabolite of DP-155 in the serum. After DP-155 oral administration, indomethacin's half-life in the serum and the brain was 22 and 93 h, respectively, compared with 10 and 24 h following indomethacin oral administration. The brain to serum ratio was 3.5 times higher for DP-155 than indomethacin. This finding explains the efficacy of DP-155 in reducing Abeta42 brain levels, despite the low systemic blood concentrations of indomethacin derived from DP-155. In conclusion, compared with indomethacin, DP-155 has significantly lower toxicity in the gut and kidney while maintaining similar efficacy to indomethacin in lowering Abeta42 in the brains of Tg2576 mice. This superior safety profile highlights DP-155's potential as an improved indomethacin-based therapy for AD." @default.
- W2110196989 created "2016-06-24" @default.
- W2110196989 creator A5001763159 @default.
- W2110196989 creator A5011083210 @default.
- W2110196989 creator A5025756017 @default.
- W2110196989 creator A5029193787 @default.
- W2110196989 creator A5030236919 @default.
- W2110196989 creator A5032790555 @default.
- W2110196989 creator A5042503074 @default.
- W2110196989 creator A5045835004 @default.
- W2110196989 creator A5064978611 @default.
- W2110196989 creator A5065946973 @default.
- W2110196989 creator A5075335478 @default.
- W2110196989 creator A5077786258 @default.
- W2110196989 creator A5078116328 @default.
- W2110196989 date "2006-06-08" @default.
- W2110196989 modified "2023-10-15" @default.
- W2110196989 title "A Novel Phospholipid Derivative of Indomethacin, DP-155 [Mixture of 1-Steroyl and 1-Palmitoyl-2-{6-[1-(<i>p</i>-chlorobenzoyl)-5-methoxy-2-methyl-3-indolyl acetamido]hexanoyl}-<i>sn</i>-glycero-3-phosophatidyl Choline], Shows Superior Safety and Similar Efficacy in Reducing Brain Amyloid β in an Alzheimer's Disease Model" @default.
- W2110196989 cites W1862355269 @default.
- W2110196989 cites W1929267935 @default.
- W2110196989 cites W1971739558 @default.
- W2110196989 cites W1972163358 @default.
- W2110196989 cites W1973131152 @default.
- W2110196989 cites W1980769611 @default.
- W2110196989 cites W1986688921 @default.
- W2110196989 cites W1986695958 @default.
- W2110196989 cites W1988137019 @default.
- W2110196989 cites W1988590999 @default.
- W2110196989 cites W1996223952 @default.
- W2110196989 cites W1997202670 @default.
- W2110196989 cites W2001210466 @default.
- W2110196989 cites W2007254610 @default.
- W2110196989 cites W2024485081 @default.
- W2110196989 cites W2029399557 @default.
- W2110196989 cites W2048510554 @default.
- W2110196989 cites W2062159035 @default.
- W2110196989 cites W2082276462 @default.
- W2110196989 cites W2083556882 @default.
- W2110196989 cites W2095277533 @default.
- W2110196989 cites W2101077392 @default.
- W2110196989 cites W2113690827 @default.
- W2110196989 cites W2126129139 @default.
- W2110196989 cites W2171469414 @default.
- W2110196989 cites W2331006443 @default.
- W2110196989 doi "https://doi.org/10.1124/jpet.106.103184" @default.
- W2110196989 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/16763096" @default.
- W2110196989 hasPublicationYear "2006" @default.
- W2110196989 type Work @default.
- W2110196989 sameAs 2110196989 @default.
- W2110196989 citedByCount "29" @default.
- W2110196989 countsByYear W21101969892012 @default.
- W2110196989 countsByYear W21101969892014 @default.
- W2110196989 countsByYear W21101969892016 @default.
- W2110196989 countsByYear W21101969892017 @default.
- W2110196989 countsByYear W21101969892018 @default.
- W2110196989 countsByYear W21101969892020 @default.
- W2110196989 countsByYear W21101969892021 @default.
- W2110196989 countsByYear W21101969892023 @default.
- W2110196989 crossrefType "journal-article" @default.
- W2110196989 hasAuthorship W2110196989A5001763159 @default.
- W2110196989 hasAuthorship W2110196989A5011083210 @default.
- W2110196989 hasAuthorship W2110196989A5025756017 @default.
- W2110196989 hasAuthorship W2110196989A5029193787 @default.
- W2110196989 hasAuthorship W2110196989A5030236919 @default.
- W2110196989 hasAuthorship W2110196989A5032790555 @default.
- W2110196989 hasAuthorship W2110196989A5042503074 @default.
- W2110196989 hasAuthorship W2110196989A5045835004 @default.
- W2110196989 hasAuthorship W2110196989A5064978611 @default.
- W2110196989 hasAuthorship W2110196989A5065946973 @default.
- W2110196989 hasAuthorship W2110196989A5075335478 @default.
- W2110196989 hasAuthorship W2110196989A5077786258 @default.
- W2110196989 hasAuthorship W2110196989A5078116328 @default.
- W2110196989 hasConcept C126322002 @default.
- W2110196989 hasConcept C134018914 @default.
- W2110196989 hasConcept C185592680 @default.
- W2110196989 hasConcept C2777056448 @default.
- W2110196989 hasConcept C2777477808 @default.
- W2110196989 hasConcept C2780026642 @default.
- W2110196989 hasConcept C2780306776 @default.
- W2110196989 hasConcept C2780664492 @default.
- W2110196989 hasConcept C29730261 @default.
- W2110196989 hasConcept C71924100 @default.
- W2110196989 hasConcept C98274493 @default.
- W2110196989 hasConceptScore W2110196989C126322002 @default.
- W2110196989 hasConceptScore W2110196989C134018914 @default.
- W2110196989 hasConceptScore W2110196989C185592680 @default.
- W2110196989 hasConceptScore W2110196989C2777056448 @default.
- W2110196989 hasConceptScore W2110196989C2777477808 @default.
- W2110196989 hasConceptScore W2110196989C2780026642 @default.
- W2110196989 hasConceptScore W2110196989C2780306776 @default.
- W2110196989 hasConceptScore W2110196989C2780664492 @default.
- W2110196989 hasConceptScore W2110196989C29730261 @default.
- W2110196989 hasConceptScore W2110196989C71924100 @default.
- W2110196989 hasConceptScore W2110196989C98274493 @default.
- W2110196989 hasIssue "3" @default.
- W2110196989 hasLocation W21101969891 @default.
- W2110196989 hasLocation W21101969892 @default.
- W2110196989 hasOpenAccess W2110196989 @default.