- Tytuł:
- Biological evaluation of [18F]-nifedipine as a novel PET tracer for L-type calcium channel imaging
- Autorzy:
-
Sadeghpour, H.
Jalilian, A. R.
Akhlaghi, M.
Shafiee, A.
Mirzaii, M.
Miri, R.
Saddadi, F. - Powiązania:
- https://bibliotekanauki.pl/articles/147732.pdf
- Data publikacji:
- 2008
- Wydawca:
- Instytut Chemii i Techniki Jądrowej
- Tematy:
-
dihydropyridines
flourine-18
PET
biodistribution - Opis:
- Due to interesting role of dihydropyridines in cardiovascular diseases and drug resistance studies and lack of a fluorine-18 labeled imaging agent for L-type calcium channel studies, this study was designed. [18F]Dimethyl 2-(fluoromethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 2 was prepared in no-carrier-added (n.c.a.) form from a starting brominated compound in one step at 80°C in Kryptofix2.2.2/[18F]. Compound 2 was administered to normal rats via their tail veins for preliminary biodistribution studies and the ID/g% of the labeled compound was determined up to 3 h post injections. Coincidence images were obtained in rats 5 to 120 min. Radiofluorination on bromo precursor gave a fluorinated compound in 95% radiochemical purity and a 8% yield shown by RTLC and HPLC. Biodistribution studies showed that the tracer is accumulated in the heart in the first few minutes, followed by metabolism resulting in very soluble 18F-containing metabolites eliminated through the urinary tract. In coincidence images, the target organ was shown to be the heart. Lung had high accumulation possibly due to the presence of Ca2+ channels and/or hydrolyzing enzymes showing a significant myocardial uptake at 120 min. The data demonstrates a significant agreement with the reported L-type calcium channels throughout the animal body. To our knowledge, this is the first example of 18F-DHPs in the literature.
- Źródło:
-
Nukleonika; 2008, 53, 4; 151-154
0029-5922
1508-5791 - Pojawia się w:
- Nukleonika
- Dostawca treści:
- Biblioteka Nauki
Artykuł