Preparation of no-carrier-added [124I]A14-iodoinsulin as a radiotracer for positron emission tomography

Matthias Glaser, David J. Brown, Marilyn P. Law, Patricia Iozzo, Stephen L. Waters, Keith Poole, Markus Knickmeier, Paolo G. Camici, Victor W. Pike

Research output: Contribution to journalArticlepeer-review


A14-Iodoinsulin is a close biochemical and pharmacological mimic of insulin. Human insulin was labelled in its A chain tyrosine-14 residue by direct iodination with the positron-emitter iodine-124 (β+ = 25.6%; t1/2 = 4.15 days) to provide a radiotracer for imaging with positron emission tomography (PET). Several reagents were compared for conversion of cyclotron-produced [124I]iodide into a reactive species for the labelling reaction. Radiochemical yields from the use of Iodo-Gen®, Chloramine-T, N-bromosuccinimide or lactoperoxidase-hydrogen peroxide were similar [35% (n = 1), 33 ± 9% (n = 10), 32 ± 11% (n = 25) or 33% (n = 2), respectively]. [124I]A14-Iodoinsulin was separated from unreacted insulin and radioactive by-products by tandem reverse phase HPLC and rapidly formulated for intravenous injection by adsorption on a Sep-Pak tC18-Plus® cartridge, followed by elution with 10 mM hydrochloric acid-ethanol (1:1 v/v, 1 ml). This radiotracer can now be obtained in useful radioactivities at high effective specific radioactivity and is now being applied to PET studies of its biodistribution in living subjects.

Original languageEnglish
Pages (from-to)465-480
Number of pages16
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Issue number6
Publication statusPublished - 2001


  • Human insulin
  • Iodine-124
  • Iodine-125
  • Iodoinsulin
  • PET
  • Specific radioactivity

ASJC Scopus subject areas

  • Analytical Chemistry
  • Drug Discovery
  • Organic Chemistry
  • Clinical Biochemistry
  • Molecular Medicine
  • Pharmacology


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