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.
• Języki publikacji: EN

Abstrakty

EN

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.

Słowa kluczowe

EN

dihydropyridines; flourine-18; PET; biodistribution

• Wydawca: Institute of Nuclear Chemistry and Technology
• Czasopismo: Nukleonika
• Rocznik: 2008
• Tom: Vol. 53, No. 4
• Strony: 151--154
• Opis fizyczny: Bibliogr. 14 poz., rys.

Twórcy

autor

Sadeghpour H.

autor

Jalilian A. R.

autor

Akhlaghi M.

autor

Shafiee A.

autor

Mirzaii M.

autor

Miri R.

autor

Saddadi F.

• Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, P. O. Box 14155-6451, Tehran, Iran and Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research School (AMIRS-NSTRI), P.

Bibliografia

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