FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2076598960> ?p ?o ?g. }

• W2076598960 endingPage "212" @default.
• W2076598960 startingPage "203" @default.
• W2076598960 abstract "High-affinity iodine- and ethyl-C-5 substituted analogs of 4-hydroxy-3-(3-[11C]methoxyphenyl)-2(1H)-quinolone ([11C]4HQ) were synthesized as new positron emission tomography radioligands for the glycine-binding sites of the N-methyl-d-aspartate (NMDA) ion channel. Although both radioligands showed high in vitro specific binding to rat brain slices, their binding characteristics were quite different from each other. 5-Ethyl-[11C]4HQ (5Et-[11C]4HQ) showed higher in vitro binding in the forebrain regions than in the cerebellum, bindings that were strongly inhibited by both glycine-site agonists and antagonists. In contrast, 5-iodo-[11C]4HQ (5I-[11C]4HQ) showed a homogeneous in vitro binding throughout the brain, which was inhibited by antagonists but not by agonists. This difference in in vitro binding between 5Et-[11C]4HQ and 5I-[11C]4HQ was quite similar to that previously observed between [11C]L-703,717 and [11C]4HQ, both glycine-site antagonists. In vivo brain uptakes of these 11C-labeled 4-hydroxyquinolones were examined in mice. Initial brain uptakes of 5Et- and 5I-[11C]4HQ at 1 min after intravenous injections were comparable to that of [11C]4HQ, but they were 1.3-2.1 times higher than that of [11C]L-703,717. The treatment with an anticoagulant, warfarin, only slightly increased the initial uptakes of [11C]4HQ and 5Et-[11C]4HQ in contrast to [11C]L-703,717. The in vivo regional brain distributions were slightly different between the two radioligands. Pretreatment with nonradioactive ligand (2 mg/kg) slightly inhibited the binding of 5Et-[11C]4HQ (16-36% inhibition) but not that of 5I-[11C]4HQ. In this study, it was found that a small structural change in [11C]4HQ resulted in a major change in binding characteristics and distributions, suggesting the existence of two binding sites for [11C]4-hydroxyquinolones on the NMDA ion channel - agonist-sensitive and agonist-insensitive (or antagonist-preferring) sites." @default.
• W2076598960 created "2016-06-24" @default.
• W2076598960 creator A5005744122 @default.
• W2076598960 creator A5010220365 @default.
• W2076598960 creator A5035030146 @default.
• W2076598960 creator A5045802956 @default.
• W2076598960 creator A5050418287 @default.
• W2076598960 creator A5054317005 @default.
• W2076598960 creator A5057832404 @default.
• W2076598960 creator A5069248010 @default.
• W2076598960 creator A5075433231 @default.
• W2076598960 creator A5076133971 @default.
• W2076598960 creator A5085113555 @default.
• W2076598960 creator A5085556975 @default.
• W2076598960 creator A5085824381 @default.
• W2076598960 creator A5087175752 @default.
• W2076598960 date "2008-02-01" @default.
• W2076598960 modified "2023-10-17" @default.
• W2076598960 title "Difference in brain distributions of carbon 11-labeled 4-hydroxy-2(1H)-quinolones as PET radioligands for the glycine-binding site of the NMDA ion channel" @default.
• W2076598960 cites W1974728184 @default.
• W2076598960 cites W1974737879 @default.
• W2076598960 cites W1975275982 @default.
• W2076598960 cites W1978079999 @default.
• W2076598960 cites W1978171643 @default.
• W2076598960 cites W1993838739 @default.
• W2076598960 cites W1997225413 @default.
• W2076598960 cites W1999818541 @default.
• W2076598960 cites W2001358308 @default.
• W2076598960 cites W2002518521 @default.
• W2076598960 cites W2008714592 @default.
• W2076598960 cites W2017991212 @default.
• W2076598960 cites W2027315266 @default.
• W2076598960 cites W2028133023 @default.
• W2076598960 cites W2034234742 @default.
• W2076598960 cites W2039695709 @default.
• W2076598960 cites W2042031554 @default.
• W2076598960 cites W2043780424 @default.
• W2076598960 cites W2045455782 @default.
• W2076598960 cites W2051503121 @default.
• W2076598960 cites W2053980736 @default.
• W2076598960 cites W2059334396 @default.
• W2076598960 cites W2061100444 @default.
• W2076598960 cites W2075345533 @default.
• W2076598960 cites W2079545833 @default.
• W2076598960 cites W2088790808 @default.
• W2076598960 cites W2108727722 @default.
• W2076598960 cites W2148035249 @default.
• W2076598960 cites W2153689707 @default.
• W2076598960 cites W2156042340 @default.
• W2076598960 cites W2185500017 @default.
• W2076598960 doi "https://doi.org/10.1016/j.nucmedbio.2007.10.007" @default.
• W2076598960 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/18312830" @default.
• W2076598960 hasPublicationYear "2008" @default.
• W2076598960 type Work @default.
• W2076598960 sameAs 2076598960 @default.
• W2076598960 citedByCount "10" @default.
• W2076598960 countsByYear W20765989602012 @default.
• W2076598960 countsByYear W20765989602014 @default.
• W2076598960 countsByYear W20765989602015 @default.
• W2076598960 countsByYear W20765989602018 @default.
• W2076598960 countsByYear W20765989602020 @default.
• W2076598960 countsByYear W20765989602023 @default.
• W2076598960 crossrefType "journal-article" @default.
• W2076598960 hasAuthorship W2076598960A5005744122 @default.
• W2076598960 hasAuthorship W2076598960A5010220365 @default.
• W2076598960 hasAuthorship W2076598960A5035030146 @default.
• W2076598960 hasAuthorship W2076598960A5045802956 @default.
• W2076598960 hasAuthorship W2076598960A5050418287 @default.
• W2076598960 hasAuthorship W2076598960A5054317005 @default.
• W2076598960 hasAuthorship W2076598960A5057832404 @default.
• W2076598960 hasAuthorship W2076598960A5069248010 @default.
• W2076598960 hasAuthorship W2076598960A5075433231 @default.
• W2076598960 hasAuthorship W2076598960A5076133971 @default.
• W2076598960 hasAuthorship W2076598960A5085113555 @default.
• W2076598960 hasAuthorship W2076598960A5085556975 @default.
• W2076598960 hasAuthorship W2076598960A5085824381 @default.
• W2076598960 hasAuthorship W2076598960A5087175752 @default.
• W2076598960 hasConcept C107824862 @default.
• W2076598960 hasConcept C116569031 @default.
• W2076598960 hasConcept C150903083 @default.
• W2076598960 hasConcept C170493617 @default.
• W2076598960 hasConcept C185592680 @default.
• W2076598960 hasConcept C202751555 @default.
• W2076598960 hasConcept C207001950 @default.
• W2076598960 hasConcept C2777756961 @default.
• W2076598960 hasConcept C515207424 @default.
• W2076598960 hasConcept C55493867 @default.
• W2076598960 hasConcept C67018056 @default.
• W2076598960 hasConcept C71240020 @default.
• W2076598960 hasConcept C86803240 @default.
• W2076598960 hasConceptScore W2076598960C107824862 @default.
• W2076598960 hasConceptScore W2076598960C116569031 @default.
• W2076598960 hasConceptScore W2076598960C150903083 @default.
• W2076598960 hasConceptScore W2076598960C170493617 @default.
• W2076598960 hasConceptScore W2076598960C185592680 @default.
• W2076598960 hasConceptScore W2076598960C202751555 @default.
• W2076598960 hasConceptScore W2076598960C207001950 @default.
• W2076598960 hasConceptScore W2076598960C2777756961 @default.

• next