title: Synthesis and biological evaluation of 68Ga labeled bis-DOTA-3,3'-(benzylidene)-bis-(1H-indole-2-carbohydrazide) as a PET tracer for in vivo visualization of necrosis.
abstract: The aim of the present study was to develop a (68)Ga labeled bis-DOTA derivative of benzylidene-bis-indole and compare the in vivo stability and biodistribution with that of the previously reported bis-DTPA derivate for in vivo imaging of necrosis using PET. Uptake of the tracer was evaluated in a mouse model of Fas-mediated hepatic apoptosis in correlation with histochemical stainings. The novel (68)Ga labeled tracer showed an improved in vivo stability and could therefore be used for selective non-invasive imaging of necrotic cell death using PET.
authors: KU Leuven Department of Pharmaceutical & Pharmacological Sciences, Laboratory of Radiopharmacy, Herestraat 49, Box 821, BE-3000 Leuven, Belgium.
authors: Kristof
authors: K
authors: Prinsen
authors: Marlein Miranda
authors: MM
authors: Cona
authors: Jan
authors: J
authors: Cleynhens
authors: Hubert
authors: H
authors: Vanbilloen
authors: Junjie
authors: J
authors: Li
authors: Natalia
authors: N
authors: Dyubankova
authors: Eveline
authors: E
authors: Lescrinier
authors: Guy
authors: G
authors: Bormans
authors: Yicheng
authors: Y
authors: Ni
authors: Alfons
authors: A
authors: Verbruggen
mesh_terms: D000818:Animals; D017209:Apoptosis / Q000187:drug effects; D056831:Coordination Complexes / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000633:toxicity; D005710:Gallium Radioisotopes / Q000737:chemistry; D006207:Half-Life; D006573:Heterocyclic Compounds, 1-Ring / Q000737:chemistry*; D051379:Mice; D009336:Necrosis / Q000000981:diagnostic imaging*; D004369:Pentetic Acid / Q000737:chemistry; D049268:Positron-Emission Tomography; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000633:toxicity; D014018:Tissue Distribution / Q000187:drug effects; D019014:fas Receptor / Q000378:metabolism
chemical_list: D056831:Coordination Complexes; C491899:Fas protein, mouse; D005710:Gallium Radioisotopes; D006573:Heterocyclic Compounds, 1-Ring; D019275:Radiopharmaceuticals; D019014:fas Receptor; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid; D004369:Pentetic Acid