NDLI: A Triazacyclononane-Based Bifunctional Phosphinate Ligand for the Preparation of Multimeric $^{68}Ga$ Tracers for Positron Emission Tomography

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A Triazacyclononane-Based Bifunctional Phosphinate Ligand for the Preparation of Multimeric $^{68}Ga$ Tracers for Positron Emission Tomography

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A Triazacyclononane-Based Bifunctional Phosphinate Ligand for the Preparation of Multimeric $^{68}Ga$ Tracers for Positron Emission Tomography

Content Provider	World Health Organization (WHO)-Global Index Medicus
Author	Lukes, Ivan Kubícek, Vojtech Havlícková, Jana Hermann, Petr Plutnar, Jan Loktionova, Natalia Rösch, Frank Kotek, Jan Notni, Johannes Riss, Patrick Johannes
Description	Author Affiliation: Notni J ( Department of Nuclear Medicine, Technische Universität München, Ismaninger Str. 22, 81675 München, Germany. johannes.notni@tum.de)
Abstract	For application in positron emission tomography (PET), PrP9, a N,N′,N′′-trisubstituted triazacyclononane with methyl(2-carboxyethyl)phosphinic acid pendant arms, was developed as $^{68}Ga^{3+}$ complexing agent. The synthesis is short and inexpensive. $Ga^{III}$ and $Fe^{III}$ complexes of PrP9 were characterized by single-crystal X-ray diffraction. Stepwise protonation constants and thermodynamic stabilities of metal complexes were determined by potentiometry. The $Ga^{III}$ complex possesses a high thermodynamic stability $(log K_{[GaL]}=26.24)$ and a high degree of kinetic inertness. $^{68}Ga$ labeling of PrP9 is possible at ambient temperature and in a wide pH range, also at pH values as low as 1. This means that for the first time, the neat eluate of a $TiO_{2}-based$ $^{68}Ge/^{68}Ga$ generator (typically consisting of 0.1 M HCl) can be directly used for labeling purposes. The rate of $^{68}Ga$ activity incorporation at pH 3.3 and 20 °C is higher than for the established chelators DOTA and NOTA. Tris-amides of PrP9 with amino acid esters were synthesized to act as models for multimeric peptide conjugates. These conjugates exhibit radiolabeling properties similar to those of unsubstituted PrP9.
ISSN	09476539
e-ISSN	15213765
Journal	Chemistry - A European Journal
Issue Number	24
Volume Number	16
Language	English
Publisher	Wiley-VCH;ChemPubSoc Europe
Publisher Date	2010-06-25
Publisher Place	Germany
Access Restriction	Open
Subject Keyword	Gallium Isotopes Chemistry Macrocyclic Compounds Organometallic Compounds Phosphinic Acids Positron-Emission Tomography Isotope Labeling Ligands Molecular Structure Radiopharmaceuticals X-Ray Diffraction Research Support, Non-U.S. Gov't
Content Type	Text
Resource Type	Article
Subject	Organic Chemistry Catalysis

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A Triazacyclononane-Based Bifunctional Phosphinate Ligand for the Preparation of Multimeric $^{68}Ga$ Tracers for Positron Emission Tomography

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