Synthesis of carbon-11-labeled bivalent Β-carbolines as new PET agents for imaging of cholinesterase in Alzheimer's disease

Min Wang, David X. Zheng, Mingzhang Gao, Gary D. Hutchins, Qi Huang Zheng

Research output: Contribution to journalArticlepeer-review

6 Scopus citations

Abstract

Carbon-11-labeled bivalent Β-carbolines, 9,9'-(pentane-1,5-diyl)bis(2-[11C]methyl-9H-pyrido[3,4-b]indol-2-ium)iodide ([11C]2a), 9,9'-(nonane-1,9-diyl)bis(2-[11C]methyl-9H-pyrido[3,4-b]indol-2-ium)iodide ([11C]2b), 9,9'-(dodecane-1,12-diyl)bis(2-[11C]methyl-9H-pyrido[3,4-b]indol-2-ium)iodide ([11C]2c) and 1,9-bis(2-[11C]methyl-3,4-dihydro-1H-pyrido[3,4-b]indol-9(2H)-yl)nonane ([11C]3), were prepared by N-[11C]methylation of their corresponding amine precursors using [11C]CH3I and isolated by either a simplified solid-phase extraction (SPE) method or HPLC in 40-60% radiochemical yields based on [11C]CO2 and decay corrected to end of bombardment (EOB). The overall synthesis time from EOB was 20-30min, the radiochemical purity was >99%, and the specific activity at end of synthesis (EOS) was 185-370GBq/γmol.

Original languageEnglish (US)
Pages (from-to)678-685
Number of pages8
JournalApplied Radiation and Isotopes
Volume69
Issue number4
DOIs
StatePublished - Apr 2011

Keywords

  • Alzheimer's disease
  • Carbon-11-labeled bivalent Β-carbolines
  • Cholinesterase
  • Imaging
  • Positron emission tomography

ASJC Scopus subject areas

  • Radiation

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