Exploration of Sulfur‐Containing Analogues for Imaging Vesicular Acetylcholine Transporter in the Brain

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‐fluor...

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Veröffentlicht in:	ChemMedChem 2018-09, Vol.13 (18), p.1978-1987
Hauptverfasser:	Luo, Zonghua, Liu, Hui, Jin, Hongjun, Gu, Jiwei, Yu, Yanbo, Kaneshige, Kota, Perlmutter, Joel S., Parsons, Stanley M., Tu, Zhude
Format:	Artikel
Sprache:	eng
Schlagworte:	Accumulation Acetylcholine Affinity Animals Autoradiography Binding biodistribution Blood-Brain Barrier - drug effects Blood-Brain Barrier - metabolism Brain Brain - drug effects Brain - metabolism Dose-Response Relationship, Drug Enantiomers Humans In vivo methods and tests Kinetics Ligands Molecular Structure Neostriatum neurodegenerative diseases Neuroimaging positron emission tomography Radioactive tracers Radiopharmaceuticals - chemistry Radiopharmaceuticals - metabolism Radiopharmaceuticals - pharmacokinetics radiotracers Rats Rats, Sprague-Dawley Receptors Structure-Activity Relationship Sulfur Sulfur - chemistry Tissue Distribution Vesamicol Vesicular Acetylcholine Transport Proteins - analysis Vesicular Acetylcholine Transport Proteins - antagonists & inhibitors Vesicular Acetylcholine Transport Proteins - metabolism Vesicular acetylcholine transporter
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