2018
DOI: 10.1002/cmdc.201800411
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Exploration of Sulfur‐Containing Analogues for Imaging Vesicular Acetylcholine Transporter in the Brain

Abstract: Sixteen new sulfur-containing compounds targeting the vesicular acetylcholine transporter (VAChT) were synthesized and assessed for in vitro binding affinities. Enantiomers (-)-(1-(3-hydroxy-1,2,3,4-tetrahydronaphthalen-2-yl)piperidin-4-yl)(4-(methylthio)phenyl)methanone [(-)-8] and (-)-(4-((2-fluoroethyl)thio)phenyl)(1-(3-hydroxy-1,2,3,4-tetrahydronaph-thalen-2-yl)piperidin-4-yl)methanone [(-)-14 a] displayed high binding affinities, with respective K values of 1.4 and 2.2 nm for human VAChT, moderate and hig… Show more

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Cited by 4 publications
(1 citation statement)
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“…The intermediate 1-[ 18 F]fluoro-2tosyloxyethane was radiosynthesized following the published procedure. 43,54,56 A solution of precursor 31 (3-4 mg) and Cs 2 CO 3 (2-3 mg) in DMSO (200 mL) was added to the reaction vessel containing 1-[ 18 F]fluoro-2-tosyloxyethane. The vessel was capped and heated at 110 °C for 15 min.…”
Section: Papermentioning
confidence: 99%
“…The intermediate 1-[ 18 F]fluoro-2tosyloxyethane was radiosynthesized following the published procedure. 43,54,56 A solution of precursor 31 (3-4 mg) and Cs 2 CO 3 (2-3 mg) in DMSO (200 mL) was added to the reaction vessel containing 1-[ 18 F]fluoro-2-tosyloxyethane. The vessel was capped and heated at 110 °C for 15 min.…”
Section: Papermentioning
confidence: 99%