Internalization of radiolabelled [DTPA0]octreotide and [DOTA0,Tyr3]octreotide: peptides for somatostatin receptor-targeted scintigraphy and radionuclide therapy

Nucl Med Commun. 1998 Mar;19(3):283-8. doi: 10.1097/00006231-199803000-00013.

Abstract

We compared the internalization of [90Y-DOTA0,Tyr3]octreotide and [111In-DOTA0,Tyr3]octreotide with that of [125I-Tyr3]octreotide and [111In-DTPA0]octreotide in the subtype 2 somatostatin receptor (sst2)-positive rat pancreatic tumour cell lines CA20948 and AR42J and in the somatostatin receptor-negative human anaplastic thyroid tumour cell line ARO. We demonstrated that [111In-DTPA0]octreotide, [90Y-DOTA0,Tyr3]octreotide and [111In-DOTA0,Tyr3]octreotide are internalized by a receptor-specific, time- and temperature-dependent process. The amount of [90Y-DOTA0,Tyr3]octreotide internalized was higher than that of [111In-DOTA0,Tyr3]octreotide and [111In-DTPA0]octreotide.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Binding, Competitive
  • Biological Transport
  • Carcinoma / metabolism
  • Cell Line
  • Humans
  • Indium Radioisotopes / pharmacokinetics
  • Kinetics
  • Octreotide / analogs & derivatives
  • Octreotide / pharmacokinetics*
  • Pancreatic Neoplasms / metabolism*
  • Pentetic Acid / analogs & derivatives
  • Pentetic Acid / pharmacokinetics*
  • Radiopharmaceuticals / pharmacokinetics*
  • Rats
  • Receptors, Somatostatin / metabolism*
  • Temperature
  • Thyroid Neoplasms / metabolism*
  • Tumor Cells, Cultured
  • Yttrium Radioisotopes / pharmacokinetics

Substances

  • Indium Radioisotopes
  • Radiopharmaceuticals
  • Receptors, Somatostatin
  • Yttrium Radioisotopes
  • Pentetic Acid
  • Octreotide