title: Radiolabeling and preliminary biological evaluation of a (99m)Tc(CO)(3) labeled 3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) derivative as a potential SPECT tracer for in vivo visualization of necrosis.
abstract: N,N'-bis(diethylenetriamine pentaacetic acid)-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) (bis-DTPA-BI) was radiolabeled with (99m)Tc(CO)(3). The resulting (99m)Tc(CO)(3)-bis-DTPA-BI was characterized (LC-MS) and evaluated as a potential SPECT tracer for imaging of necrosis in Wistar rats with a reperfused partial liver infarction and Wistar rats with ethanol induced muscular necrosis. To study the specificity, uptake of (99m)Tc(CO)(3)-bis-DTPA-BI was also studied in a mouse model of Fas-mediated hepatic apoptosis. The obtained results indicate that (99m)Tc(CO)(3)-bis-DTPA-BI displays selective uptake in necrotic tissue and can be used for in vivo visualization of necrosis by SPECT.
authors.affiliation: Laboratory for Radiopharmacy, Faculty of Pharmaceutical Sciences, Katholieke Universiteit Leuven, Herestraat 49, Box 821, BE-3000 Leuven, Belgium.
authors.forename: Kristof
authors.initials: K
authors.lastname: Prinsen
authors.forename: Lixin
authors.initials: L
authors.lastname: Jin
authors.forename: Kathleen
authors.initials: K
authors.lastname: Vunckx
authors.forename: Marijke
authors.initials: M
authors.lastname: De Saint-Hubert
authors.forename: Lin
authors.initials: L
authors.lastname: Zhou
authors.forename: Jan
authors.initials: J
authors.lastname: Cleynhens
authors.forename: Johan
authors.initials: J
authors.lastname: Nuyts
authors.forename: Guy
authors.initials: G
authors.lastname: Bormans
authors.forename: Yicheng
authors.initials: Y
authors.lastname: Ni
authors.forename: Alfons
authors.initials: A
authors.lastname: Verbruggen
mesh_terms: D000818:Animals; D017209:Apoptosis; D022781:Hepatocytes / Q000473:pathology; D007211:Indoles / Q000138:chemical synthesis / Q000737:chemistry*; D007553:Isotope Labeling; D051379:Mice; D009336:Necrosis / Q000175:diagnosis*; D015609:Organotechnetium Compounds / Q000737:chemistry*; D004369:Pentetic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D007211:Indoles; C557268:N,N'-bis(diethylenetriamine pentaacetic acid)-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide); D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; D004369:Pentetic Acid