Catabolism of neurotensins. Implications for the design of radiolabeling strategies of peptides

Q J Nucl Med. 1999 Jun;43(2):155-8.

Abstract

A major impact in diagnosis and treatment of cancer with peptide based radiopharmaceuticals is expected. Among others neurotensin is considered to be a promising candidate. However, most neurotensin analogues, which bind to the neurotensin receptor have a too short biological half live due to catabolism. Therefore, stabilized fragments have been prepared and labeled with the newly developed [Tc(CO)3](+)-moiety. A single histidine or a (N alpha-His)-Ac group coupled to the N-terminus of the neurotensin fragments were used as a bidentate or a tridentate ligand respectively, which coordinate the metal carbonyl efficiently. Affinity and binding studies of the 99mTc(I) radiolabeled neurotensin fragments revealed a behavior influenced by catabolism and properties of the metal complex.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Affinity Labels
  • Binding Sites
  • Half-Life
  • Histidine / analogs & derivatives
  • Histidine / chemistry
  • Humans
  • Ligands
  • Neoplasms / diagnostic imaging
  • Neoplasms / radiotherapy
  • Neurotensin / analogs & derivatives
  • Neurotensin / chemistry
  • Neurotensin / metabolism*
  • Neurotensin / pharmacokinetics
  • Organotechnetium Compounds / chemical synthesis
  • Organotechnetium Compounds / chemistry
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis*
  • Radiopharmaceuticals / chemistry
  • Receptors, Neurotensin / metabolism

Substances

  • Affinity Labels
  • Ligands
  • Organotechnetium Compounds
  • Radiopharmaceuticals
  • Receptors, Neurotensin
  • Neurotensin
  • Histidine