AAZTA: An Ideal Chelating Agent for the Development of 44Sc PET Imaging Agents1. Issue 8 (18th January 2017)

• Record Type: Journal Article
• Authors: Nagy, Gábor; Szikra, Dezső; Trencsényi, György; Fekete, Anikó; Garai, Ildikó; Giani, Arianna M.; Negri, Roberto; Masciocchi, Norberto; Maiocchi, Alessandro; Uggeri, Fulvio; Tóth, Imre; Aime, Silvio; Giovenzana, Giovanni B.; Baranyai, Zsolt
• Is Part Of: Angewandte Chemie international edition. Volume 56:Issue 8(2017)
• Page Start: 2118
• Page End: 2122
• Publication Date: 2017-01-18
• Subjects: kinetics -- PET -- radiopharmaceuticals -- scandium -- thermodynamics; Chemistry -- Periodicals; 540
• DOI: 10.1002/anie.201611207
• Languages: English
• ISSNs: 1433-7851

Abstract

Abstract: Unprecedented fast and efficient complexation of Sc III was demonstrated with the chelating agent AAZTA (AAZTA=1, 4‐bis(carboxymethyl)‐6‐[bis(carboxymethyl)]amino‐6‐methylperhydro‐1, 4‐diazepine) under mild experimental conditions. The robustness of the 44 Sc(AAZTA) − chelate and conjugated biomolecules thereof is further shown by in vivo PET imaging in healthy and tumor mice models. The new results pave the way towards development of efficient Sc‐based radiopharmaceuticals using the AAZTA chelator. Abstract : AAZTA (1, 4‐bis(carboxymethyl)‐6‐[bis(carboxymethyl)]amino‐6‐methylperhydro‐1, 4‐diazepine) is a promising chelator for scandium‐based radiopharmaceuticals owing to high thermodynamic stability, kinetic inertness, and fast formation kinetics of the complexes. AAZTA allows 44 Sc‐radiolabeled (bio)conjugates to be prepared under mild conditions, taking full advantage of the wide time window offered by the 44 Sc isotope. (RCY=radiochemical yield).