title: Ga(III) chelates of amphiphilic DOTA-based ligands: synthetic route and in vitro and in vivo studies.
abstract: In this work, we report on a synthetic strategy using amphiphilic DOTA (1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid)-based chelators bearing a variable-sized α-alkyl chain at one of the pendant acetate arms (from 6 to 14 carbon atoms), compatible with their covalent coupling to amine-bearing biomolecules. The amphiphilic behavior of the micelles-forming Ga(III) chelates (critical micellar concentration), their stability in blood serum and their lipophilicity (logP) were investigated. Biodistribution studies with the (67)Ga-labeled chelates were performed in Wistar rats, which showed a predominant liver uptake with almost no traces of the radiochelates in the body after 24 h.
authors.affiliation: Centro de Química, Campus de Gualtar, Universidade do Minho, 4710-057 Braga, Portugal.
authors.forename: André
authors.initials: A
authors.lastname: Fontes
authors.forename: M Isabel M
authors.initials: MI
authors.lastname: Prata
authors.forename: Carlos F G C
authors.initials: CF
authors.lastname: Geraldes
authors.forename: João P
authors.initials: JP
authors.lastname: André
mesh_terms: D000818:Animals; D002614:Chelating Agents / Q000737:chemistry*; D005710:Gallium Radioisotopes / Q000737:chemistry; D006573:Heterocyclic Compounds, 1-Ring / Q000097:blood / Q000138:chemical synthesis* / Q000737:chemistry* / Q000493:pharmacokinetics; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D008024:Ligands; D008297:Male; D008823:Micelles; D051381:Rats; D017208:Rats, Wistar
chemical_list: D002614:Chelating Agents; D005710:Gallium Radioisotopes; D006573:Heterocyclic Compounds, 1-Ring; D008024:Ligands; D008823:Micelles; C071349:1,4,7,10-tetraazacyclododecane- 1,4,7,10-tetraacetic acid