An Improved Antagonist Radiotracer for the κ-Opioid Receptor: Synthesis and Characterization of (11)C-LY2459989.

ABSTRACT:

Unlabelled

The κ-opioid receptors (KORs) are implicated in several neuropsychiatric diseases and addictive disorders. PET with radioligands provides a means to image the KOR in vivo and investigate its function in health and disease. The purpose of this study was to develop the selective KOR antagonist (11)C-LY2459989 as a PET radioligand and characterize its imaging performance in nonhuman primates.

Methods

LY2459989 was synthesized and assayed for in vitro binding to opioid receptors. Ex vivo studies in rodents were conducted to assess its potential as a tracer candidate. (11)C-LY2459989 was synthesized by reaction of its iodophenyl precursor with (11)C-cyanide, followed by partial hydrolysis of the resulting (11)C-cyanophenyl intermediate. Imaging experiments with (11)C-L

SUBMITTER: Zheng MQ 

PROVIDER: S-EPMC4826283 | biostudies-literature | 2014 Jul

REPOSITORIES: biostudies-literature