title: Internalization of radiolabelled [DTPA0]octreotide and [DOTA0,Tyr3]octreotide: peptides for somatostatin receptor-targeted scintigraphy and radionuclide therapy.
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.
authors.affiliation: Department of Nuclear Medicine, University Hospital Dijkzigt, Rotterdam, The Netherlands.
authors.forename: M
authors.initials: M
authors.lastname: De Jong
authors.forename: B F
authors.initials: BF
authors.lastname: Bernard
authors.forename: E
authors.initials: E
authors.lastname: De Bruin
authors.forename: A
authors.initials: A
authors.lastname: Van Gameren
authors.forename: W H
authors.initials: WH
authors.lastname: Bakker
authors.forename: T J
authors.initials: TJ
authors.lastname: Visser
authors.forename: H R
authors.initials: HR
authors.lastname: Mäcke
authors.forename: E P
authors.initials: EP
authors.lastname: Krenning
mesh_terms: D000818:Animals; D001667:Binding, Competitive; D001692:Biological Transport; D002277:Carcinoma / Q000378:metabolism; D002460:Cell Line; D006801:Humans; D007205:Indium Radioisotopes / Q000493:pharmacokinetics; D007700:Kinetics; D015282:Octreotide / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D010190:Pancreatic Neoplasms / Q000378:metabolism*; D004369:Pentetic Acid / Q000031:analogs & derivatives / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000493:pharmacokinetics*; D051381:Rats; D017481:Receptors, Somatostatin / Q000378:metabolism*; D013696:Temperature; D013964:Thyroid Neoplasms / Q000378:metabolism*; D014407:Tumor Cells, Cultured; D015021:Yttrium Radioisotopes / Q000493:pharmacokinetics
chemical_list: D007205:Indium Radioisotopes; D019275:Radiopharmaceuticals; D017481:Receptors, Somatostatin; D015021:Yttrium Radioisotopes; D004369:Pentetic Acid; D015282:Octreotide