FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W2616992614> ?p ?o ?g. }

• W2616992614 endingPage "5209" @default.
• W2616992614 startingPage "5197" @default.
• W2616992614 abstract "The vesicular acetylcholine transporter (VAChT) is a reliable biomarker for assessing cholinergic dysfunction associated with dementia. We recently reported three new potent and selective carbon-11 labeled VAChT radiotracers. Herein, we report the resolution with a Chiralcel OD column of three additional fluorine containing VAChT ligands in which a fluoroethoxy or fluoroethylamino moiety was substituted for the methoxy group. An in vitro competitive binding assay showed that (−)-7 had high potency for VAChT (Ki-VAChT = 0.31 ± 0.03 nM) and excellent selectivity for VAChT versus σ receptors (Ki-σ1 = 1870 ± 250 nM, Ki-σ2 = 5480 ± 140 nM). Three different radiolabeling approaches were explored; the radiosynthesis of (−)-[18F]7 was successfully accomplished via a stepwise two-pot, three-step method with moderate yield (11 ± 2%) and high radiochemical purity (>98%). PET imaging studies in a nonhuman primate indicated that (−)-[18F]7 rapidly entered the brain and accumulated in the VAChT-enriched striatum. The uptake of (−)-[18F]7 in the target striatal area peaked at 10 min and displayed improved clearance kinetics compared to the VAChT tracer [18F]VAT, which has been approved by the Food and Drug Administration (FDA) for first-in-man studies. These studies justify further investigation of (−)-[18F]7 and exploration of the structure–activity relationships of these fluoroethoxy and fluoroethylamino analogs." @default.
• W2616992614 created "2017-06-05" @default.
• W2616992614 creator A5015429223 @default.
• W2616992614 creator A5031804038 @default.
• W2616992614 creator A5036528352 @default.
• W2616992614 creator A5050656056 @default.
• W2616992614 creator A5053731803 @default.
• W2616992614 creator A5061153948 @default.
• W2616992614 creator A5070606018 @default.
• W2616992614 creator A5085708878 @default.
• W2616992614 creator A5089327014 @default.
• W2616992614 date "2017-01-01" @default.
• W2616992614 modified "2023-09-25" @default.
• W2616992614 title "Synthesis, resolution, and in vitro evaluation of three vesicular acetylcholine transporter ligands and evaluation of the lead fluorine-18 radioligand in a nonhuman primate" @default.
• W2616992614 cites W1275434546 @default.
• W2616992614 cites W144871696 @default.
• W2616992614 cites W1498633126 @default.
• W2616992614 cites W1898037648 @default.
• W2616992614 cites W1950580375 @default.
• W2616992614 cites W1971783082 @default.
• W2616992614 cites W1983197298 @default.
• W2616992614 cites W1987790473 @default.
• W2616992614 cites W1992430378 @default.
• W2616992614 cites W1992982129 @default.
• W2616992614 cites W1999191328 @default.
• W2616992614 cites W1999638333 @default.
• W2616992614 cites W2016560512 @default.
• W2616992614 cites W2036195467 @default.
• W2616992614 cites W2038555389 @default.
• W2616992614 cites W2064111465 @default.
• W2616992614 cites W2068493805 @default.
• W2616992614 cites W2073818021 @default.
• W2616992614 cites W2074359179 @default.
• W2616992614 cites W2074521340 @default.
• W2616992614 cites W2074631079 @default.
• W2616992614 cites W2087485448 @default.
• W2616992614 cites W2089052849 @default.
• W2616992614 cites W2093431193 @default.
• W2616992614 cites W2094483441 @default.
• W2616992614 cites W2096855081 @default.
• W2616992614 cites W2114190954 @default.
• W2616992614 cites W2115889677 @default.
• W2616992614 cites W2142052067 @default.
• W2616992614 cites W2147540551 @default.
• W2616992614 cites W2154360214 @default.
• W2616992614 cites W2171289971 @default.
• W2616992614 cites W2189722612 @default.
• W2616992614 cites W2267188822 @default.
• W2616992614 cites W2317970953 @default.
• W2616992614 cites W2318096101 @default.
• W2616992614 cites W2414077889 @default.
• W2616992614 cites W587214412 @default.
• W2616992614 doi "https://doi.org/10.1039/c7ob00854f" @default.
• W2616992614 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/5561660" @default.
• W2616992614 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/28590490" @default.
• W2616992614 hasPublicationYear "2017" @default.
• W2616992614 type Work @default.
• W2616992614 sameAs 2616992614 @default.
• W2616992614 citedByCount "6" @default.
• W2616992614 countsByYear W26169926142018 @default.
• W2616992614 countsByYear W26169926142020 @default.
• W2616992614 countsByYear W26169926142022 @default.
• W2616992614 crossrefType "journal-article" @default.
• W2616992614 hasAuthorship W2616992614A5015429223 @default.
• W2616992614 hasAuthorship W2616992614A5031804038 @default.
• W2616992614 hasAuthorship W2616992614A5036528352 @default.
• W2616992614 hasAuthorship W2616992614A5050656056 @default.
• W2616992614 hasAuthorship W2616992614A5053731803 @default.
• W2616992614 hasAuthorship W2616992614A5061153948 @default.
• W2616992614 hasAuthorship W2616992614A5070606018 @default.
• W2616992614 hasAuthorship W2616992614A5085708878 @default.
• W2616992614 hasAuthorship W2616992614A5089327014 @default.
• W2616992614 hasBestOaLocation W26169926142 @default.
• W2616992614 hasConcept C150903083 @default.
• W2616992614 hasConcept C169760540 @default.
• W2616992614 hasConcept C185592680 @default.
• W2616992614 hasConcept C198399640 @default.
• W2616992614 hasConcept C202751555 @default.
• W2616992614 hasConcept C207001950 @default.
• W2616992614 hasConcept C22885893 @default.
• W2616992614 hasConcept C2775910092 @default.
• W2616992614 hasConcept C2776970183 @default.
• W2616992614 hasConcept C2777731756 @default.
• W2616992614 hasConcept C55493867 @default.
• W2616992614 hasConcept C67847695 @default.
• W2616992614 hasConcept C71240020 @default.
• W2616992614 hasConcept C71924100 @default.
• W2616992614 hasConcept C86803240 @default.
• W2616992614 hasConcept C98274493 @default.
• W2616992614 hasConceptScore W2616992614C150903083 @default.
• W2616992614 hasConceptScore W2616992614C169760540 @default.
• W2616992614 hasConceptScore W2616992614C185592680 @default.
• W2616992614 hasConceptScore W2616992614C198399640 @default.
• W2616992614 hasConceptScore W2616992614C202751555 @default.
• W2616992614 hasConceptScore W2616992614C207001950 @default.
• W2616992614 hasConceptScore W2616992614C22885893 @default.
• W2616992614 hasConceptScore W2616992614C2775910092 @default.
• W2616992614 hasConceptScore W2616992614C2776970183 @default.

• next