Development of a novel radiobromine-labeled sigma-1 receptor imaging probe

Sigma-1 receptor is a target for tumor imaging. In a previous study, we synthesized a vesamicol analog, (+)-2-[4-(4-bromophenyl)piperidino]cyclohexanol [(+)-pBrV], with a high affinity for sigma-1 receptor, and synthesized radiobrominated (+)-pBrV. This radiobrominated (+)-pBrV showed high tumor uptake in tumor-bearing mice; however, radioactivity accumulation in normal tissues, such as the liver, was high. We assumed that the accumulation of (+)-pBrV in the non-target tissues was partially derived from its high lipophilicity; therefore, we synthesized and evaluated (+)-4-[1-(2-hydroxycyclohexyl)piperidine-4-yl]-2-bromophenol [(+)-BrV-OH], which is a more hydrophilic compound.

Source: Nuclear Medicine and Biology - April 6, 2018 Category: Nuclear Medicine Authors: Kazuma Ogawa, Ryohei Masuda, Yoshiaki Mizuno, Akira Makino, Takashi Kozaka, Yoji Kitamura, Yasushi Kiyono, Kazuhiro Shiba, Akira Odani Source Type: research