Syntheses and in vitro evaluation of decalinvesamicol analogues as potential imaging probes for vesicular acetylcholine transporter (VAChT)

T Kozaka, I Uno, Y Kitamura, D Miwa, K Ogawa…

Index: Kozaka, Takashi; Uno, Izumi; Kitamura, Yoji; Miwa, Daisuke; Ogawa, Kazuma; Shiba, Kazuhiro Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 16 p. 4936 - 4941

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Citation Number: 9

Abstract

A series of vesamicol analogues, o-iodo-trans-decalinvesamicol (OIDV) or o-bromo-trans- decalinvesamicol (OBDV), were synthesized and their affinities to vesicular acetylcholine transporter (VAChT) and σ receptors (σ-1, σ-2) were evaluated by in vitro binding assays using rat cerebral or liver membranes. OIDV and OBDV showed greater binding affinity to VAChT (Ki= 20.5±5.6 and 13.8±1.2 nM, respectively) than did vesamicol (Ki= 33.9±18.1 ...