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Biological evaluation of [18F]-nifedipine as a novel PET tracer for L-type calcium channel imaging

Sadeghpour H., Jalilian A. R., Akhlaghi M., Shafiee A., Mirzaii M., Miri R., Saddadi F.

Nukleonika

2008

Vol. 53, No. 4

151-154

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.

Preparation and biodistribution of [201Tl](III)vancomycin complex in normal rats

Jalilian A., Hosseini M., Karimian A., Saddadi F., Sadeghi M.

Nukleonika

2006

Vol. 51, nr 4

203-208

Thallium-201 (T1/2 = 3.04 days) in Tl+ form was converted to Tl3+ cation in presence of O3 in 6 M HCl controlled by RTLC/gel electrophoresis methods. The final evaporated activity was reacted with vancomycin (VAN) in water to yield [201Tl](III)VAN. The best results were obtained at room temperature in water after 30 min with a radiochemical yield > 99%, after mixing the reactants followed by SPE purification using Si Sep-Pak. The studies showed that thallic ion is mostly incorporated into vancomycin with a radiochemical purity of more than 98 š 1% by RTLC. A specific activity of about 4.14 x 1010 Bq/mmol was obtained. Radiochemical purity and stability of 201Tl-VAN in the preparation and in presence of human serum was determined up to 5.5 days. Biodistribution study of 201Tl(III)-vancomycin in normal rats was performed up to 52 h.