FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2127830324> ?p ?o ?g. }

• W2127830324 endingPage "185" @default.
• W2127830324 startingPage "177" @default.
• W2127830324 abstract "[Carbonyl-11C]WAY-100635 ([11C]WAY) is an established radioligand for the study of brain serotonin1A (5-HT1A) receptors in living animals and humans with positron emission tomography (PET). There is a recognised need to develop halogenated ligands for 5-HT1A receptors, either for labelling with longer-lived fluorine-18 for more widespread application with PET or with iodine-123 for application with single photon emission tomography (SPET). Here we used autoradiography and PET to assess two new halogenated anlogues of WAY, namely 6BPWAY and 6FPWAY [N-(2-(1-(4-(2-methoxyphenyl)-piperazinyl)ethyl))-N-(2-(6-bromo-/fluoro-pyridinyl))cyclohexanecarboxamide] as prospective radioligands, initially using carbon-11 as the radiolabel. Labelling of 6BPWAY and 6FPWAY with carbon-11 was accomplished by acylation of the corresponding secondary amine precursors with [carbonyl-11C]cyclohexanecarbonyl chloride. After incubation of human brain crysections with [11C]6BPWAY or [11C]6FPWAY, the highest accumulation of radioactivity was observed in cortical areas and the hippocampal formation. Both radioligands had high nonspecific binding. There was a rapid accumulation of radioactivity in the monkey brain after intravenous injection of [11C]6BPWAY and [11C]6FPWAY. High accumulation of radioactivity was observed in the frontal and temporal cortex and the raphe nuclei, areas known to contain a high density of 5-HT1A receptors. The ratios of radioactivity in receptor-rich temporal cortex to that in receptor-poor cerebellum at peak equilibrium were 1.9 (at 10 min) and 3.0 at (at 20 min) for [11C]6BPWAY and [11C]6FPWAY, respectively. In pretreatment experiments with high doses of unlabelled WAY, the level of radioactivity in the frontal and temporal cortex and the raphe nuclei was reduced to the same level as in the cerebellum. Radioactive metabolites of [11C]6FPWAY appeared at a rate similar to those for [11C]WAY, with 17% of the radioactivity in plasma represented by unchanged radioligand after 40 min. Radioactive metabolites of [11C]6BPWAY appeared much more slowly. At 40 min after injection 45% of the radioactivity in plasma still represented unchanged radioligand. The results indicate that 6-pyridinyl radiohalogented analogues of WAY are new leads to radioligands for PET or SPET." @default.
• W2127830324 created "2016-06-24" @default.
• W2127830324 creator A5002184470 @default.
• W2127830324 creator A5026079546 @default.
• W2127830324 creator A5030118197 @default.
• W2127830324 creator A5036179587 @default.
• W2127830324 creator A5038622526 @default.
• W2127830324 creator A5044969808 @default.
• W2127830324 creator A5048937067 @default.
• W2127830324 creator A5061483789 @default.
• W2127830324 creator A5067222102 @default.
• W2127830324 creator A5072890433 @default.
• W2127830324 creator A5081327813 @default.
• W2127830324 date "2001-02-01" @default.
• W2127830324 modified "2023-10-15" @default.
• W2127830324 title "New halogenated [11C]WAY analogues, [11C]6FPWAY and [11C]6BPWAY—Radiosynthesis and assessment as radioligands for the study of brain 5-HT1A receptors in living monkey" @default.
• W2127830324 cites W1971547290 @default.
• W2127830324 cites W2010825915 @default.
• W2127830324 cites W2023229299 @default.
• W2127830324 cites W2028435242 @default.
• W2127830324 cites W2039240477 @default.
• W2127830324 cites W2042304831 @default.
• W2127830324 cites W2043897751 @default.
• W2127830324 cites W2050451612 @default.
• W2127830324 cites W2051065313 @default.
• W2127830324 cites W2052094195 @default.
• W2127830324 cites W2054426856 @default.
• W2127830324 cites W2054676102 @default.
• W2127830324 cites W2060285943 @default.
• W2127830324 cites W2067068908 @default.
• W2127830324 cites W2068483106 @default.
• W2127830324 cites W2089686687 @default.
• W2127830324 cites W2113084435 @default.
• W2127830324 cites W2114177397 @default.
• W2127830324 cites W2131593240 @default.
• W2127830324 cites W2164700562 @default.
• W2127830324 cites W2166461470 @default.
• W2127830324 cites W2170943825 @default.
• W2127830324 cites W2333710732 @default.
• W2127830324 cites W4231983498 @default.
• W2127830324 doi "https://doi.org/10.1016/s0969-8051(00)00181-5" @default.
• W2127830324 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/11295428" @default.
• W2127830324 hasPublicationYear "2001" @default.
• W2127830324 type Work @default.
• W2127830324 sameAs 2127830324 @default.
• W2127830324 citedByCount "27" @default.
• W2127830324 countsByYear W21278303242012 @default.
• W2127830324 countsByYear W21278303242013 @default.
• W2127830324 countsByYear W21278303242014 @default.
• W2127830324 countsByYear W21278303242017 @default.
• W2127830324 countsByYear W21278303242019 @default.
• W2127830324 countsByYear W21278303242020 @default.
• W2127830324 countsByYear W21278303242022 @default.
• W2127830324 countsByYear W21278303242023 @default.
• W2127830324 crossrefType "journal-article" @default.
• W2127830324 hasAuthorship W2127830324A5002184470 @default.
• W2127830324 hasAuthorship W2127830324A5026079546 @default.
• W2127830324 hasAuthorship W2127830324A5030118197 @default.
• W2127830324 hasAuthorship W2127830324A5036179587 @default.
• W2127830324 hasAuthorship W2127830324A5038622526 @default.
• W2127830324 hasAuthorship W2127830324A5044969808 @default.
• W2127830324 hasAuthorship W2127830324A5048937067 @default.
• W2127830324 hasAuthorship W2127830324A5061483789 @default.
• W2127830324 hasAuthorship W2127830324A5067222102 @default.
• W2127830324 hasAuthorship W2127830324A5072890433 @default.
• W2127830324 hasAuthorship W2127830324A5081327813 @default.
• W2127830324 hasConcept C15744967 @default.
• W2127830324 hasConcept C169760540 @default.
• W2127830324 hasConcept C170493617 @default.
• W2127830324 hasConcept C177322064 @default.
• W2127830324 hasConcept C185592680 @default.
• W2127830324 hasConcept C2775842073 @default.
• W2127830324 hasConcept C2776970183 @default.
• W2127830324 hasConcept C2780523633 @default.
• W2127830324 hasConcept C2989005 @default.
• W2127830324 hasConcept C2993858690 @default.
• W2127830324 hasConcept C55493867 @default.
• W2127830324 hasConcept C67847695 @default.
• W2127830324 hasConcept C71924100 @default.
• W2127830324 hasConceptScore W2127830324C15744967 @default.
• W2127830324 hasConceptScore W2127830324C169760540 @default.
• W2127830324 hasConceptScore W2127830324C170493617 @default.
• W2127830324 hasConceptScore W2127830324C177322064 @default.
• W2127830324 hasConceptScore W2127830324C185592680 @default.
• W2127830324 hasConceptScore W2127830324C2775842073 @default.
• W2127830324 hasConceptScore W2127830324C2776970183 @default.
• W2127830324 hasConceptScore W2127830324C2780523633 @default.
• W2127830324 hasConceptScore W2127830324C2989005 @default.
• W2127830324 hasConceptScore W2127830324C2993858690 @default.
• W2127830324 hasConceptScore W2127830324C55493867 @default.
• W2127830324 hasConceptScore W2127830324C67847695 @default.
• W2127830324 hasConceptScore W2127830324C71924100 @default.
• W2127830324 hasIssue "2" @default.
• W2127830324 hasLocation W21278303241 @default.
• W2127830324 hasLocation W21278303242 @default.
• W2127830324 hasOpenAccess W2127830324 @default.
• W2127830324 hasPrimaryLocation W21278303241 @default.
• W2127830324 hasRelatedWork W1971543955 @default.

• next