Synthesis and in vitro evaluation of new benzovesamicol analogues as potential imaging probes for the vesicular acetylcholine transporter

Y Zea-Ponce, S Mavel, T Assaad, SE Kruse…

文献索引：Zea-Ponce, Yolanda; Mavel, Sylvie; Assaad, Thaer; Kruse, Shane E.; Parsons, Stanley M.; Emond, Patrick; Chalon, Sylvie; Giboureau, Nicolas; Kassiou, Michael; Guilloteau, Denis Bioorganic and Medicinal Chemistry, 2005 , vol. 13, # 3 p. 745 - 753

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被引用次数: 36

摘要

Our goal was to synthesize new stereospecific benzovesamicol analogues, which could potentially be used as SPECT or PET radioligands for the vesicular acetylcholine transporter (VAChT). This paper describes the chemical synthesis, resolution and determination of binding affinity for four enantiomeric pairs of derivatives. Their intrinsic affinities were determined by competition against binding of [3H] vesamicol to human VAChT. Of the ...