0000000001001044

AUTHOR

Bradley P. Waldron

showing 4 related works from this author

Equilibrium, Kinetic and Structural Properties of Gallium(III) and Some Divalent Metal Complexes Formed with the New DATAm and DATA5m Ligands

2017

The development of 68Ge/68Ga generators has made the positron-emitting 68Ga isotope widely accessible and raised interest in new chelate complexes of Ga3+. The hexadentate 1,4-di(acetate)-6-methyl[amino(methyl)acetate]perhydro-1,4-diazepane (DATAm) ligand and its bifunctional analogue, 1,4-di(acetate)-6-pentanoic acid[amino(methyl)acetate]perhydro-1,4-diazepane (DATA5m), rapidly form complexes with 68Ga in high radiochemical yield. The stability constants of DATAm and DATA5m complexes formed with Ga3+, Zn2+, Cu2+, Mn2+ and Ca2+ have been determined by using pH potentiometry, spectrophotometry (Cu2+) and 1H and 71Ga NMR spectroscopy (Ga3+). The stability constants of Ga(DATAm) and Ga(DATA5m)…

Reaction mechanism010405 organic chemistryLigandOrganic ChemistryInorganic chemistrychemistry.chemical_elementGeneral ChemistryNuclear magnetic resonance spectroscopy010402 general chemistry01 natural sciencesMedicinal chemistryCatalysisDissociation (chemistry)0104 chemical scienceschemistry.chemical_compoundTransmetalationchemistryTermészettudományokChelationGalliumBifunctionalKémiai tudományok
researchProduct

Structure and stability of hexadentate complexes of ligands based on AAZTA for efficient PET labelling with gallium-68

2012

Pre-organised tricarboxylate ligands based on 6-amino-perhydro-1,4-diazepine bind (68)Ga rapidly and selectively in acetate buffer at pH 4 to 7, forming kinetically stable complexes suitable for use in PET imaging.

ChemistryMetals and Alloyschemistry.chemical_elementGeneral ChemistryPet imagingTricarboxylateCombinatorial chemistryCatalysisSurfaces Coatings and FilmsElectronic Optical and Magnetic MaterialsLabellingMaterials ChemistryCeramics and CompositesOrganic chemistryGalliumChem. Commun.
researchProduct

Approaching ‘kit-type’ labelling with 68Ga : the DATA chelators.

2015

The DATA chelators are a novel class of tri-anionic ligands based on 6-amino-1,4-diazepine-triacetic acid, which have been introduced recently for the chelation of (68)Ga. Compared with macrocyclic chelators based on the cyclen scaffold (i.e., DOTA, DO3A, and DO2A derivatives), DATA chelators undergo quantitative radiolabelling more rapidly and under milder conditions. In this study, a systematic evaluation of the labelling of four DATA chelators--DATA(M), DATA(P), DATA(Ph), and DATA(PPh)--with (68)Ga is presented. The results highlight the extraordinary potential of this new class of chelators for application in molecular imaging using (68)Ga positron emission tomography (PET).

PharmacologyStereochemistryRadiopharmaceuticals.Organic ChemistryGallium-68Gallium RadioisotopesBiochemistryLigand designchemistry.chemical_compoundKineticsMacrocyclic ligandsCyclenchemistryLabellingIsotope LabelingDrug DiscoveryChelatesMolecular MedicineDOTAChelationGeneral Pharmacology Toxicology and PharmaceuticsMolecular imagingChelating Agents
researchProduct

Instant kit preparation of 68Ga-radiopharmaceuticals via the hybrid chelator DATA: clinical translation of [68Ga]Ga-DATA-TOC

2019

Purpose The widespread use of 68Ga for positron emission tomography (PET) relies on the development of radiopharmaceutical precursors that can be radiolabelled and dispensed in a simple, quick, and convenient manner. The DATA (6-amino-1,4-diazapine-triacetate) scaffold represents a novel hybrid chelator architecture possessing both cyclic and acyclic character that may allow for facile access to 68Ga-labelled tracers in the clinic. We report the first bifunctional DATA chelator conjugated to [Tyr3]octreotide (TOC), a somatostatin subtype 2 receptor (SST2)-targeting vector for imaging and functional characterisation of SSTR2 expressing tumours. Methods The radiopharmaceutical precursor, DATA…

lcsh:Medical physics. Medical radiology. Nuclear medicineNET540 Chemistry and allied sciencesDOTA-TOC540 Chemielcsh:R895-920Gallium-68PET-CTDATA-TOCMolecular imagingOriginal ResearchSomatostatin receptorEJNMMI Research
researchProduct