In vitro and in vivo evaluation of new radiolabeled neurotensin(8-13) analogues with high affinity for NT1 receptors

Nucl Med Biol. 2001 Jan;28(1):75-84. doi: 10.1016/s0969-8051(00)00190-6.

Abstract

The potential utility of neurotensin (NT) in cancer diagnosis and therapy is limited by its rapid degradation. New stabilized analogues were synthesized, labeled with [99mTc] and screened in vitro and in vivo. High affinity and rapid internalization were obtained in binding assays. Despite their longer human plasma half-lives, a rapid degradation was observed with low concentrations as used in biodistribution tests. The tumor uptake rates were rather low but tumor/blood ratios increased according to the stability raise.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Chromatography, High Pressure Liquid
  • Drug Stability
  • HT29 Cells / metabolism
  • Half-Life
  • Humans
  • Mice
  • Mice, Nude
  • Neurotensin / analogs & derivatives*
  • Neurotensin / chemical synthesis
  • Neurotensin / metabolism
  • Neurotensin / pharmacokinetics*
  • Peptide Fragments / pharmacokinetics*
  • Radiopharmaceuticals / chemical synthesis
  • Radiopharmaceuticals / metabolism
  • Radiopharmaceuticals / pharmacokinetics*
  • Receptors, Neurotensin / metabolism*
  • Structure-Activity Relationship
  • Tissue Distribution

Substances

  • Peptide Fragments
  • Radiopharmaceuticals
  • Receptors, Neurotensin
  • Neurotensin
  • neurotensin (8-13)