4.4 Article

Radiosynthesis of N-[11C]-methyl-hydroxyfasudil as a new potential PET radiotracer for rho-kinases (ROCKs)

Journal

APPLIED RADIATION AND ISOTOPES
Volume 68, Issue 2, Pages 325-328

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.apradiso.2009.11.002

Keywords

Carbon-11; Fasudil; Hydroxyfasudil; Rho-kinases; Intracellular labeling

Funding

  1. Heart and Stroke Foundation Molecular Function and Imaging [6242]

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N-[C-11]-methyl-hydroxyfasudil was synthesized as a new potential radiotracer for rho-kinases (ROCKS) via a two-step one-pot radiosynthesis. The first step was the methylation of the precursor N-Boc-hydroxyfasudil-sodium salt/benzo-15-crown-5 complex with [C-11]methyl iodide. The second step involved deprotection of the tert-butoxycarbonyl protecting group. The radiochemical and chemical purities of N-[C-11]-methyl-hydroxyfasudil were >95% and specific radioactivity was 1565-2565 mCi/mu mol at the end of the synthesis. (C) 2009 Elsevier Ltd. All rights reserved.

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