Parameter evaluation and fully-automated radiosynthesis of [(11)C]harmine for imaging of MAO-A for clinical trials

Appl Radiat Isot. 2015 Mar:97:182-187. doi: 10.1016/j.apradiso.2015.01.002. Epub 2015 Jan 7.

Abstract

The aim of the present study was the evaluation and automation of the radiosynthesis of [(11)C]harmine for clinical trials. The following parameters have been investigated: amount of base, precursor concentration, solvent, reaction temperature and time. The optimum reaction conditions were determined to be 2-3mg/mL precursor activated with 1eq. 5M NaOH in DMSO, 80°C reaction temperature and 2min reaction time. Under these conditions 6.1±1GBq (51.0±11% based on [(11)C]CH3I, corrected for decay) of [(11)C]harmine (n=72) were obtained. The specific activity was 101.32±28.2GBq/µmol (at EOS). All quality control parameters were in accordance with the standards for parenteral human application. Due to its reliability and high yields, this fully-automated synthesis method can be used as routine set-up.

Keywords: Carbon-11; MAO-A; Monoamine oxidase; PET; Radiosynthesis; [(11)C]harmine.

Publication types

  • Evaluation Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Brain / diagnostic imaging
  • Brain / enzymology
  • Carbon Radioisotopes* / standards
  • Chemistry Techniques, Synthetic / instrumentation
  • Chemistry Techniques, Synthetic / methods
  • Clinical Trials as Topic
  • Harmine / chemical synthesis*
  • Harmine / standards
  • Humans
  • Monoamine Oxidase / metabolism*
  • Positron-Emission Tomography
  • Quality Control
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / standards

Substances

  • Carbon Radioisotopes
  • Radiopharmaceuticals
  • Harmine
  • Monoamine Oxidase
  • monoamine oxidase A, human