In vitro and in vivo evaluation of new radiolabeled neurotensin(8-13) analogues with high affinity for NT1 receptors.
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.
García-Garayoa
E
E
Paul Scherrer Institute, Centre for Radiopharmaceutical Science, Ch-5232 PSI, Villigen, Switzerland.
Allemann-Tannahill
L
L
Bläuenstein
P
P
Willmann
M
M
Carrel-Rémy
N
N
Tourwé
D
D
Iterbeke
K
K
Conrath
P
P
Schubiger
P A
PA
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
D010446:Peptide Fragments; D019275:Radiopharmaceuticals; D018028:Receptors, Neurotensin; D009496:Neurotensin; C054381:neurotensin (8-13)