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RESEARCH PRODUCT
Radiolabelling and preliminary evaluation of 68Ga-tetrapyrrole derivatives as potential tracers for PET
Elisabeth EppardFrederic ZollerFrank RöschFranz-peter MontfortsPatrick J. RissPatrick J. RissDebra K. Kellehersubject
MaleCancer Researchmedicine.medical_treatmentGallium RadioisotopesPhotodynamic therapyEndocytosischemistry.chemical_compoundDrug StabilityRadioligandmedicineAnimalsHumansRadiology Nuclear Medicine and imagingRadiochemistrymedicine.diagnostic_testRadiochemistryBlood ProteinsPorphyrinTetrapyrroleIn vitroRatsTetrapyrroleschemistryBiochemistryPositron emission tomographyIsotope LabelingPositron-Emission TomographyMolecular MedicineRadionuclide Generatordescription
article i nfo Tetrapyrroles are multisided natural products which are of relevance in clinical medicine. Owing to their specific accumulation in tumour tissue, porphyrins, metalloporphyrins and chlorins have been used as in photodynamic therapy and optical imaging. Moreover, their specific uptake into inflammatory atheromatous plaques via LDL endocytosis has been reported. The present study is concerned with the synthesis of 68 Ga labelled porphyrin derivatives and an in vitro assessment of the utility of radiotracers in positron emission tomography. A set of five porphyrin derivatives were labelled using 68 Ga from a commercially obtained radionuclide generator. Dedicated post-processing of the generator eluate was conducted to allow for labelling in aqueous media and also under anhydrous conditions. Challenge studies and incubation in human serum confirmed the stability of the tracers. Plasma protein binding was investigated in order to confirm the presence of freely diffusible radioligand in plasma. A preliminary microPET study in a tumour-bearing rat resulted in a clear visualisation of the tumour.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2013-02-01 | Nuclear Medicine and Biology |