99mTc(CO)3-VIP analogues: preparation and evaluation as tumor imaging agent

Appl Radiat Isot. 2007 Apr;65(4):382-6. doi: 10.1016/j.apradiso.2006.11.001. Epub 2006 Dec 27.

Abstract

Vasoactive intestinal peptide (VIP) receptors are expressed abundantly on many types of tumors and, hence, radiolabeled VIP analogues are being explored for tumor imaging and therapy. Here, we report synthesis of three VIP analogues and their radiolabeling with (99m)Tc via a novel tricarbonyl synthon. The radiolabeled product could be prepared in high yields (>95%) and stability. In vitro studies showed significant uptake of (99m)Tc(CO)((3))-VP05 in human colon carcinoma cells. Biodistribution studies in animal tumor model showed 0.4-1%ID/g tumor uptake.

Publication types

  • Evaluation Study

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Colonic Neoplasms / diagnostic imaging*
  • Humans
  • Isotope Labeling
  • Mice
  • Organotechnetium Compounds / chemical synthesis*
  • Organotechnetium Compounds / pharmacokinetics
  • Radionuclide Imaging
  • Vasoactive Intestinal Peptide / analogs & derivatives*
  • Vasoactive Intestinal Peptide / chemical synthesis
  • Vasoactive Intestinal Peptide / pharmacokinetics

Substances

  • Organotechnetium Compounds
  • techentium 99m tricarbonyl VD5 peptide
  • technetium 99m tricarbonyl VD4 peptide
  • technetium 99m tricarbonyl VP05 peptide
  • Vasoactive Intestinal Peptide