title: Preliminary biological evaluation of novel (99m)Tc-Cys-annexin A5 as a apoptosis imaging agent.
abstract: A novel annexin A5 derivative (cys-annexin A5) with a single cysteine residue at its C-terminal has been developed and successfully labeled in high labeling yield with (99m)Tc by a ligand exchange reaction. Like the 1st generation (99m)Tc-HYNIC-annexin A5, the novel (99m)Tc-cys-annexin A5 derivative shows in normal mice mainly renal and, to a lesser extent, hepatobiliary excretion. In rat models of hepatic apoptosis there was 283% increase in hepatic uptake of (99m)Tc-cys-annexin A5 as compared to normal mice. The results indicate that the novel (99m)Tc-cys-annexin A5 is a potential apoptosis imaging agent.
authors.affiliation: Key Laboratory of Nuclear Medicine, Ministry of Health & Jiangsu Key Laboratory of Molecular Nuclear Medicine, Jiangsu Institute of Nuclear Medicine, Wuxi 214063, China.
authors.forename: Chunxiong
authors.initials: C
authors.lastname: Lu
authors.forename: Quanfu
authors.initials: Q
authors.lastname: Jiang
authors.forename: Minjin
authors.initials: M
authors.lastname: Hu
authors.forename: Cheng
authors.initials: C
authors.lastname: Tan
authors.forename: Yu
authors.initials: Y
authors.lastname: Ji
authors.forename: Huixin
authors.initials: H
authors.lastname: Yu
authors.forename: Zichun
authors.initials: Z
authors.lastname: Hua
mesh_terms: D000818:Animals; D017304:Annexin A5 / Q000737:chemistry; D017302:Annexins / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D017209:Apoptosis; D020287:In Situ Nick-End Labeling; D007553:Isotope Labeling; D008099:Liver / Q000378:metabolism / Q000473:pathology; D008297:Male; D051379:Mice; D015609:Organotechnetium Compounds / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D019275:Radiopharmaceuticals / Q000737:chemistry* / Q000493:pharmacokinetics / Q000633:toxicity; D051381:Rats; D014018:Tissue Distribution; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D017304:Annexin A5; D017302:Annexins; D015609:Organotechnetium Compounds; D019275:Radiopharmaceuticals; C585198:technetium 99m Cys-annexin A5