Labeled Alginate Conjugates For Molecular Imaging Applications

摘要

Described are bifunctional NOTA-based derivatives capable of conjugating with alginate and with metal ions, as well as NOTA-alginate conjugates which can be labeled with stable or radioactive metal ions. Also described are conjugation methods of the bifunctional NOTA-based linker with alginate, and methods of using radiometal-labeled NOTA-alginate conjugates or other radio-labeled alginate conjugates as imaging reagents.

主权项

1. An alginate conjugate having the formula: wherein X is —(CH2)mC(O)—, with m being 1, 2, or 3; L is a linker selected from the group consisting of: wherein n, n′ and n″ are each independently a number from 0 to 10; Alg is alginic acid or an alginate salt; and Y is a spacer directly attached to the reducing end unit of alginate or the carboxyl groups of the alginate polymer chain via the active nitrogen, and has the following structure: wherein R is selected from the group consisting of hydrogen, alkyl, benzyl or an aromatic group; or a pharmaceutically acceptable salt or solvate thereof; and, wherein the alginate conjugate comprises a metal ion chelated by the 1,4,7-triazacyclononane-1,4,7-triacetic acid moiety.