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SHR Neuro Krebs Kardio Lipid Stoffw Microb
Kvaternik, H; Wanek, T; Hammerschmidt, F; Zolle, I; Aigner, R; Kuntner, C.
Radiosynthesis of [124I]iodometomidate and biological evaluation using small-animal PET.
Mol Imaging Biol. 2014; 16(3):317-321
Doi: 10.1007/s11307-013-0696-x
Web of Science
PubMed
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FullText_MUG
- Führende Autor*innen der Med Uni Graz
- Kvaternik Herbert
- Co-Autor*innen der Med Uni Graz
- Aigner Reingard
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- Abstract:
- The application of radiolabelled inhibitors of cytochrome P450 enzymes is a novel approach for molecular imaging of adrenocortical masses to detect adrenal tumours. One potential tracer is radiolabelled iodometomidate (IMTO) with a common option for scintigraphic diagnosis and therapeutic applications. The aim of this study was to radiolabel iodometomidate with the positron-emitting radionuclide iodine-124 ((124)I) for the investigation of the biological behaviour and pharmacokinetics with positron emission tomography (PET). [(124)I]IMTO has been synthesized by oxidative radioiodo-destannylation, purified via semi-preparative HPLC and formulated in acetate-buffered saline, which contained ascorbic acid and ethanol to avoid radiolytic decomposition. Biological evaluation was performed in rats which received 5.5 ± 0.7 MBq [(124)I]IMTO in vivo. The radioactivity distribution (n = 3) has been dynamically imaged from 0-120 min after intravenous (i.v.) injection by small-animal PET. Regions of interest have been defined manually in the reconstructed PET images, and the activity concentration was expressed as percent injected dose per gram tissue (%ID/g). [(124)I]IMTO was prepared with a radiochemical yield of 83 ± 5 % (n = 3) and a radiochemical purity of >97 %. The final formulation of [(124)I]IMTO was stable for up to 48 h at room temperature. Two hours after i.v. administration in rats, radioactivity concentration in the adrenal glands were 2.1 ± 0.3 %ID/g, which was sufficient to achieve highest-contrast adrenal PET images. In the present study, the biological characteristics of radioiodinated metomidate were evaluated. [(124)I]IMTO appears as an attractive PET tracer for imaging of adrenals.
- Find related publications in this database (using NLM MeSH Indexing)
- Animals -
- Etomidate - analogs & derivatives
- Etomidate - chemical synthesis
- Etomidate - pharmacokinetics
- Etomidate - pharmacology
- Female -
- Iodine Radioisotopes - chemistry
- Positron-Emission Tomography - methods
- Rats -
- Rats, Sprague-Dawley -
- Tissue Distribution -
- Find related publications in this database (Keywords)
- Metomidate
- Iodine-124
- Stability
- Small-animal PET
- Adrenal imaging