title: In vitro and in vivo evaluation of new radiolabeled neurotensin(8-13) analogues with high affinity for NT1 receptors.
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.
authors.affiliation: Paul Scherrer Institute, Centre for Radiopharmaceutical Science, Ch-5232 PSI, Villigen, Switzerland.
authors.forename: E
authors.initials: E
authors.lastname: García-Garayoa
authors.forename: L
authors.initials: L
authors.lastname: Allemann-Tannahill
authors.forename: P
authors.initials: P
authors.lastname: Bläuenstein
authors.forename: M
authors.initials: M
authors.lastname: Willmann
authors.forename: N
authors.initials: N
authors.lastname: Carrel-Rémy
authors.forename: D
authors.initials: D
authors.lastname: Tourwé
authors.forename: K
authors.initials: K
authors.lastname: Iterbeke
authors.forename: P
authors.initials: P
authors.lastname: Conrath
authors.forename: P A
authors.initials: PA
authors.lastname: Schubiger
mesh_terms: D000818:Animals; D002851:Chromatography, High Pressure Liquid; D004355:Drug Stability; D019073:HT29 Cells / Q000378:metabolism; D006207:Half-Life; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D009496:Neurotensin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D010446:Peptide Fragments / Q000493:pharmacokinetics*; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000378:metabolism / Q000493:pharmacokinetics*; D018028:Receptors, Neurotensin / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014018:Tissue Distribution
chemical_list: D010446:Peptide Fragments; D019275:Radiopharmaceuticals; D018028:Receptors, Neurotensin; D009496:Neurotensin; C054381:neurotensin (8-13)