(99m)TC-branched-chain-polypeptide (BCP): A potential synthetic radiopharmaceutical

Alan C. Perkins, Malcolm Frier, Malcolm V. Pimm, Ferenc Hudecz

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

Synthetic polymers and polypeptides are currently being investigated as a basis for a new generation of radiopharmaceuticals which do not rely on the availability of human blood products or animal derived proteins. In the present study a polyanionic branched chain polypeptide (BCP) based on a poly(L-lysine) backbone with DL-Ala oligomer side chains (three residues on average) terminating in acetylated glutamic acid (AcEAK) was conjugated to DTPA by reaction with DTPA anhydride prior to electrolytic radiolabelling with (99m)Tc. The radiolabelling efficiency of incorporation of (99m)Tc was between 40 and 50%. The radiochemical purity on ITLC with butanone was >90%. 10MBq (99m)Tc-AcEAK were administered intravenously to normal Wistar rats and the in vivo biodistribution assessed by imaging with a gamma camera. Imaging demonstrated the distribution of (99m)Tc-AcEAK throughout the body with greatest concentration of activity in the vascular organs such as the heart and liver. Quantification from the images demonstrated 65% of the whole body activity remained at 4 hours. Focal increased uptake was also visualised in the left ear of one rat which was subsequently found to be a site of infection. This study demonstrates that (99m)Tc-BCP offers potential for use as a radiopharmaceutical for blood pool and possibly infection imaging.

Original languageEnglish
Pages (from-to)631-638
Number of pages8
JournalJournal of Labelled Compounds and Radiopharmaceuticals
Volume41
Issue number7
DOIs
Publication statusPublished - Jul 1 1998

Keywords

  • (99m)Tc
  • Branched chain polypeptides
  • Synthetic radiopharmaceuticals

ASJC Scopus subject areas

  • Analytical Chemistry
  • Biochemistry
  • Radiology Nuclear Medicine and imaging
  • Drug Discovery
  • Spectroscopy
  • Organic Chemistry

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