title: Synthesis and application of lactosylated, 99mTc chelating albumin for measurement of liver function.
abstract: Neogalactosylated and neolactosylated albumins are currently used as radiopharmaceutical agents for imaging the liver asialoglycoprotein receptors, which allows the quantification of hepatic liver function in various diseases and also in healthy liver transplant donors. We developed an original process for synthesizing a chelating neolactosylated human albumin using maleimidopropyl-lactose and maleimidopropyl-diethylene triamine pentaacetic acid (DTPA) derivatives. The lactosylated protein (LACTAL) conjugate showed excellent liver uptake compared to nonlactosylated protein and a very high signal-to-noise ratio, based on functional assessment of biodistribution in mice using (99m)Tc-scintigraphy.
authors.affiliation: Universite Paris-Sud 11, EA4046, Kremlin-Bicetre, F-94275, AP-HP, CHU de Bicetre, Le Kremlin-Bicetre, F-94275, Unite de Pharmacologie Chimique et Genetique, U640 INSERM, UMR8151 CNRS, Universite Paris Descartes, Paris, France. philippe.chaumet-riffaud@bct.aphp.fr
authors.forename: Philippe
authors.initials: P
authors.lastname: Chaumet-Riffaud
authors.forename: Ivan
authors.initials: I
authors.lastname: Martinez-Duncker
authors.forename: Anne-Laure
authors.initials: AL
authors.lastname: Marty
authors.forename: Cyrille
authors.initials: C
authors.lastname: Richard
authors.forename: Alain
authors.initials: A
authors.lastname: Prigent
authors.forename: Frederic
authors.initials: F
authors.lastname: Moati
authors.forename: Laure
authors.initials: L
authors.lastname: Sarda-Mantel
authors.forename: Daniel
authors.initials: D
authors.lastname: Scherman
authors.forename: Michel
authors.initials: M
authors.lastname: Bessodes
authors.forename: Nathalie
authors.initials: N
authors.lastname: Mignet
mesh_terms: D000818:Animals; D002614:Chelating Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D006801:Humans; D008099:Liver / Q000000981:diagnostic imaging* / Q000502:physiology*; D008111:Liver Function Tests; D008297:Male; D051379:Mice; D011877:Radionuclide Imaging; D019275:Radiopharmaceuticals / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D051381:Rats; D017208:Rats, Wistar; D012709:Serum Albumin / Q000138:chemical synthesis / Q000737:chemistry / Q000493:pharmacokinetics*; D013668:Technetium Tc 99m Aggregated Albumin / Q000737:chemistry / Q000493:pharmacokinetics*; D014018:Tissue Distribution
chemical_list: D002614:Chelating Agents; D019275:Radiopharmaceuticals; D012709:Serum Albumin; D013668:Technetium Tc 99m Aggregated Albumin; C049720:lactosylated serum albumin