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Nuclear Medicine and Biology

[11C]GR103545: novel one-pot radiosynthesis with high specific activity


PMID 21315277

Abstract

Introduction GR103545 is a potent and selective kappa-opioid receptor agonist. Previous studies in non-human primates demonstrated favorable properties of [ 11C]GR103545 as a positron emission tomography tracer for in vivo imaging of cerebral kappa-opioid receptor. Nonetheless, advancement of [ 11C]GR103545 to imaging studies in humans was hampered by difficulties of its multiple-step radiosynthesis, which produces a final product with low specific activity (SA), which in turn could induce undesirable physiological side effects resulting from the mass associated with an injected amount of radioactivity. We report herein an alternative radiosynthesis of [ 11C]GR103545 with higher SA and radiochemical yields.

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