FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2051263168> ?p ?o ?g. }

• W2051263168 endingPage "199" @default.
• W2051263168 startingPage "193" @default.
• W2051263168 abstract "Palonosetron is a 5-HT3 receptor antagonist that has demonstrated superiority in preventing both acute and delayed emesis when compared to older first generation 5-HT3 receptor antagonists. The objective of this work was to determine if palonosetron exhibits unique molecular interactions with the 5-HT3 receptor that could provide a scientific rationale for observed clinical efficacy differences. Previously, we showed that palonosetron exhibits allosteric binding and positive cooperativity to the 5-HT3 receptor in contrast to ondansetron and granisetron which exhibit simple bimolecular binding. The present work shows, through several independent experiments, that palonosetron uniquely triggers 5-HT3 receptor internalization and induces prolonged inhibition of receptor function. After 24 h incubation followed by dissociation conditions, [3H]palonosetron remained associated with whole cells but not to cell-free membranes (P < 0.001). [3H]Palonosetron's binding to cells was resistant to both protease and acid treatments designed to denature cell surface proteins suggesting that the receptor complex was inside the cells rather than at the surface. Cells pretreated with unlabeled palonosetron subsequently exhibited reduced cell surface 5-HT3 receptor binding. Palonosetron-triggered receptor internalization was visualized by confocal fluorescence microscopy using cells transfected with 5-HT3 receptor fused to enhanced cyan fluorescent protein. In contrast, granisetron and ondansetron showed minimal to no effect on receptor internalization or prolonged inhibition of receptor function. These experiments may provide a pharmacological basis for differences noted in published clinical trials comparing palonosetron to other 5-HT3 receptor antagonists." @default.
• W2051263168 created "2016-06-24" @default.
• W2051263168 creator A5013531845 @default.
• W2051263168 creator A5023686004 @default.
• W2051263168 creator A5039907732 @default.
• W2051263168 creator A5046941316 @default.
• W2051263168 creator A5048687448 @default.
• W2051263168 creator A5056312293 @default.
• W2051263168 creator A5073501391 @default.
• W2051263168 creator A5077350730 @default.
• W2051263168 creator A5078466007 @default.
• W2051263168 date "2010-01-01" @default.
• W2051263168 modified "2023-10-01" @default.
• W2051263168 title "Palonosetron triggers 5-HT3 receptor internalization and causes prolonged inhibition of receptor function" @default.
• W2051263168 cites W1507515137 @default.
• W2051263168 cites W1553513611 @default.
• W2051263168 cites W1819750950 @default.
• W2051263168 cites W1966496975 @default.
• W2051263168 cites W1973339347 @default.
• W2051263168 cites W1973930987 @default.
• W2051263168 cites W1993434718 @default.
• W2051263168 cites W2000583684 @default.
• W2051263168 cites W2012165680 @default.
• W2051263168 cites W2017659594 @default.
• W2051263168 cites W2033909159 @default.
• W2051263168 cites W2056426469 @default.
• W2051263168 cites W2058278167 @default.
• W2051263168 cites W2058410057 @default.
• W2051263168 cites W2086898945 @default.
• W2051263168 cites W2096091943 @default.
• W2051263168 cites W2115353208 @default.
• W2051263168 cites W2120978512 @default.
• W2051263168 cites W2150077308 @default.
• W2051263168 cites W2153119854 @default.
• W2051263168 cites W2155726820 @default.
• W2051263168 cites W9958541 @default.
• W2051263168 doi "https://doi.org/10.1016/j.ejphar.2009.10.002" @default.
• W2051263168 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/19836386" @default.
• W2051263168 hasPublicationYear "2010" @default.
• W2051263168 type Work @default.
• W2051263168 sameAs 2051263168 @default.
• W2051263168 citedByCount "171" @default.
• W2051263168 countsByYear W20512631682012 @default.
• W2051263168 countsByYear W20512631682013 @default.
• W2051263168 countsByYear W20512631682014 @default.
• W2051263168 countsByYear W20512631682015 @default.
• W2051263168 countsByYear W20512631682016 @default.
• W2051263168 countsByYear W20512631682017 @default.
• W2051263168 countsByYear W20512631682018 @default.
• W2051263168 countsByYear W20512631682019 @default.
• W2051263168 countsByYear W20512631682020 @default.
• W2051263168 countsByYear W20512631682021 @default.
• W2051263168 countsByYear W20512631682022 @default.
• W2051263168 countsByYear W20512631682023 @default.
• W2051263168 crossrefType "journal-article" @default.
• W2051263168 hasAuthorship W2051263168A5013531845 @default.
• W2051263168 hasAuthorship W2051263168A5023686004 @default.
• W2051263168 hasAuthorship W2051263168A5039907732 @default.
• W2051263168 hasAuthorship W2051263168A5046941316 @default.
• W2051263168 hasAuthorship W2051263168A5048687448 @default.
• W2051263168 hasAuthorship W2051263168A5056312293 @default.
• W2051263168 hasAuthorship W2051263168A5073501391 @default.
• W2051263168 hasAuthorship W2051263168A5077350730 @default.
• W2051263168 hasAuthorship W2051263168A5078466007 @default.
• W2051263168 hasConcept C12554922 @default.
• W2051263168 hasConcept C126322002 @default.
• W2051263168 hasConcept C139770010 @default.
• W2051263168 hasConcept C170493617 @default.
• W2051263168 hasConcept C185592680 @default.
• W2051263168 hasConcept C2775864247 @default.
• W2051263168 hasConcept C2776712918 @default.
• W2051263168 hasConcept C2777452722 @default.
• W2051263168 hasConcept C2780204788 @default.
• W2051263168 hasConcept C2780852908 @default.
• W2051263168 hasConcept C2780884295 @default.
• W2051263168 hasConcept C53910766 @default.
• W2051263168 hasConcept C55493867 @default.
• W2051263168 hasConcept C71924100 @default.
• W2051263168 hasConcept C86803240 @default.
• W2051263168 hasConcept C98274493 @default.
• W2051263168 hasConceptScore W2051263168C12554922 @default.
• W2051263168 hasConceptScore W2051263168C126322002 @default.
• W2051263168 hasConceptScore W2051263168C139770010 @default.
• W2051263168 hasConceptScore W2051263168C170493617 @default.
• W2051263168 hasConceptScore W2051263168C185592680 @default.
• W2051263168 hasConceptScore W2051263168C2775864247 @default.
• W2051263168 hasConceptScore W2051263168C2776712918 @default.
• W2051263168 hasConceptScore W2051263168C2777452722 @default.
• W2051263168 hasConceptScore W2051263168C2780204788 @default.
• W2051263168 hasConceptScore W2051263168C2780852908 @default.
• W2051263168 hasConceptScore W2051263168C2780884295 @default.
• W2051263168 hasConceptScore W2051263168C53910766 @default.
• W2051263168 hasConceptScore W2051263168C55493867 @default.
• W2051263168 hasConceptScore W2051263168C71924100 @default.
• W2051263168 hasConceptScore W2051263168C86803240 @default.
• W2051263168 hasConceptScore W2051263168C98274493 @default.
• W2051263168 hasIssue "2-3" @default.
• W2051263168 hasLocation W20512631681 @default.

• next