title: Radiolabelling and preliminary evaluation of 68Ga-tetrapyrrole derivatives as potential tracers for PET.
abstract: 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.
authors.affiliation: Institute of Nuclear Chemistry, University of Mainz, Fritz-Strassmann-Weg 2, 55128, Mainz, Germany.
authors.forename: Frederic
authors.initials: F
authors.lastname: Zoller
authors.forename: Patrick J
authors.initials: PJ
authors.lastname: Riss
authors.forename: Franz-Peter
authors.initials: FP
authors.lastname: Montforts
authors.forename: Debra K
authors.initials: DK
authors.lastname: Kelleher
authors.forename: Elisabeth
authors.initials: E
authors.lastname: Eppard
authors.forename: Frank
authors.initials: F
authors.lastname: Rösch
mesh_terms: D000818:Animals; D001798:Blood Proteins / Q000378:metabolism; D004355:Drug Stability; D005710:Gallium Radioisotopes; D006801:Humans; D007553:Isotope Labeling; D008297:Male; D049268:Positron-Emission Tomography / Q000379:methods*; D011854:Radiochemistry; D051381:Rats; D045725:Tetrapyrroles / Q000737:chemistry* / Q000378:metabolism / Q000493:pharmacokinetics
chemical_list: D001798:Blood Proteins; D005710:Gallium Radioisotopes; D045725:Tetrapyrroles