FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W939892842> ?p ?o ?g. }

• W939892842 endingPage "974" @default.
• W939892842 startingPage "967" @default.
• W939892842 abstract "Metabotropic glutamate subtype receptor 1 (mGluR1) is implicated in several neuropsychiatric disorders and is a target for drug development. [18F]FIMX ([18F]4-fluoro--N-methyl-N--(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide) is an effective radioligand for imaging brain mGluR1 with PET. A similarly effective radioligand with a shorter half-life would usefully allow PET studies of mGluR1 at baseline and after pharmacological or other challenge on the same day. Here we describe the preparation of [11C]FIMX for evaluation in monkey with PET. [11C]FIMX was prepared via Pd-promoted carbonylation of 1-fluoro-4-iodobenzene with [11C]carbon monoxide, aminolysis of the [11C]acyl-palladium complex with the requisite Boc-protected amine, and deprotection with HCl in THF. PET scans of [11C]FIMX injected into a monkey were performed at baseline and after preblock of mGluR1 with measurement of the arterial input function. The radiosynthesis required 42 min and gave [11C]FIMX in about 5% overall decay-corrected radiochemical yield and with a specific activity of about 100 GBq/μmol. PET in rhesus monkey at baseline showed that radioactivity peaked high in receptor-rich cerebellum and much lower in receptor-poor occipital cortex. Radioactivity in cerebellum declined to 32% of peak at 85 min. VT at baseline appeared stable in all brain regions after 60 min. Under mGluR1 pre-blocked condition, radioactivity uptake in all regions declined more rapidly to a low level. Receptor pre-block reduced VT from 13.0 to 1.5 in cerebellum and from 2.9 to 1.4 in occipital cortex. [11C]FIMX is an effective radioligand for imaging mGluR1 in monkey with PET." @default.
• W939892842 created "2016-06-24" @default.
• W939892842 creator A5022725090 @default.
• W939892842 creator A5035586136 @default.
• W939892842 creator A5039918144 @default.
• W939892842 creator A5048937067 @default.
• W939892842 creator A5054234926 @default.
• W939892842 creator A5061688680 @default.
• W939892842 creator A5076368300 @default.
• W939892842 creator A5079125204 @default.
• W939892842 creator A5080172542 @default.
• W939892842 creator A5091769570 @default.
• W939892842 date "2015-12-01" @default.
• W939892842 modified "2023-09-24" @default.
• W939892842 title "[ carbonyl - 11 C]4-Fluoro- N -methyl- N -(4-(6-(methylamino)pyrimidin-4-yl)thiazol-2-yl)benzamide ([ 11 C]FIMX) is an effective radioligand for PET imaging of metabotropic glutamate receptor 1 (mGluR1) in monkey brain" @default.
• W939892842 cites W1615495952 @default.
• W939892842 cites W1961730511 @default.
• W939892842 cites W1972183007 @default.
• W939892842 cites W1980080882 @default.
• W939892842 cites W1984387221 @default.
• W939892842 cites W1999987592 @default.
• W939892842 cites W2001121359 @default.
• W939892842 cites W2001311316 @default.
• W939892842 cites W2002820309 @default.
• W939892842 cites W2010877770 @default.
• W939892842 cites W2013784863 @default.
• W939892842 cites W2017040809 @default.
• W939892842 cites W2024567375 @default.
• W939892842 cites W2028554055 @default.
• W939892842 cites W2041821395 @default.
• W939892842 cites W2044608463 @default.
• W939892842 cites W2048709650 @default.
• W939892842 cites W2050153206 @default.
• W939892842 cites W2062567667 @default.
• W939892842 cites W2069715167 @default.
• W939892842 cites W2078789579 @default.
• W939892842 cites W2079607885 @default.
• W939892842 cites W2087566431 @default.
• W939892842 cites W2088387286 @default.
• W939892842 cites W2089922984 @default.
• W939892842 cites W2103312948 @default.
• W939892842 cites W2103839731 @default.
• W939892842 cites W2103863804 @default.
• W939892842 cites W2106335834 @default.
• W939892842 cites W2112278807 @default.
• W939892842 cites W2117891587 @default.
• W939892842 cites W2120854953 @default.
• W939892842 cites W2132256401 @default.
• W939892842 cites W2132908037 @default.
• W939892842 cites W2134726769 @default.
• W939892842 cites W2149984162 @default.
• W939892842 cites W2161165761 @default.
• W939892842 cites W2266905598 @default.
• W939892842 cites W2318994705 @default.
• W939892842 cites W2322758636 @default.
• W939892842 cites W2327978336 @default.
• W939892842 cites W2280279811 @default.
• W939892842 doi "https://doi.org/10.1016/j.nucmedbio.2015.07.006" @default.
• W939892842 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4658304" @default.
• W939892842 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26320813" @default.
• W939892842 hasPublicationYear "2015" @default.
• W939892842 type Work @default.
• W939892842 sameAs 939892842 @default.
• W939892842 citedByCount "13" @default.
• W939892842 countsByYear W9398928422016 @default.
• W939892842 countsByYear W9398928422017 @default.
• W939892842 countsByYear W9398928422019 @default.
• W939892842 countsByYear W9398928422020 @default.
• W939892842 countsByYear W9398928422021 @default.
• W939892842 crossrefType "journal-article" @default.
• W939892842 hasAuthorship W939892842A5022725090 @default.
• W939892842 hasAuthorship W939892842A5035586136 @default.
• W939892842 hasAuthorship W939892842A5039918144 @default.
• W939892842 hasAuthorship W939892842A5048937067 @default.
• W939892842 hasAuthorship W939892842A5054234926 @default.
• W939892842 hasAuthorship W939892842A5061688680 @default.
• W939892842 hasAuthorship W939892842A5076368300 @default.
• W939892842 hasAuthorship W939892842A5079125204 @default.
• W939892842 hasAuthorship W939892842A5080172542 @default.
• W939892842 hasAuthorship W939892842A5091769570 @default.
• W939892842 hasBestOaLocation W9398928422 @default.
• W939892842 hasConcept C126322002 @default.
• W939892842 hasConcept C170493617 @default.
• W939892842 hasConcept C185592680 @default.
• W939892842 hasConcept C207951395 @default.
• W939892842 hasConcept C2780231548 @default.
• W939892842 hasConcept C49051014 @default.
• W939892842 hasConcept C55493867 @default.
• W939892842 hasConcept C61174792 @default.
• W939892842 hasConcept C67847695 @default.
• W939892842 hasConcept C71240020 @default.
• W939892842 hasConcept C71924100 @default.
• W939892842 hasConcept C98274493 @default.
• W939892842 hasConceptScore W939892842C126322002 @default.
• W939892842 hasConceptScore W939892842C170493617 @default.
• W939892842 hasConceptScore W939892842C185592680 @default.
• W939892842 hasConceptScore W939892842C207951395 @default.
• W939892842 hasConceptScore W939892842C2780231548 @default.

• next