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Radiochimica Acta

International Journal for chemical aspects of nuclear science and technology

Editor-in-Chief: Qaim, Syed M.


IMPACT FACTOR 2017: 1.202

CiteScore 2017: 1.22

SCImago Journal Rank (SJR) 2017: 0.409
Source Normalized Impact per Paper (SNIP) 2017: 0.869

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2193-3405
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Volume 96, Issue 12

Issues

Radiosynthesis of dimethyl-2-[18F]-(fluoromethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate for L-type calcium channel imaging

H. Sadeghpour
  • 1 Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research Sch, Karaj, Iran
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/ A. R. Jalilian / A. Shafiee
  • 2 Tehran University of Medical Sciences, Faculty of Pharmacy and Pharmaceutical Sciences Re, Tehran, Iran
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/ M. Akhlaghi
  • 3 Nuclear Research Center for Agriculture and Medicine, Cyclotron and Nuclear Medicine Department, Karaj, Iran
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/ R. Miri
  • 4 Tehran University of Medical Sciences, Faculty of Pharmacy and Pharmaceutical Sciences Re, Tehran, Iran
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/ M. Mirzaei
  • 5 Nuclear Medicine Research Group, Agricultural, Medical and Industrial Research Sch, Karaj, Iran
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Published Online: 2009-09-25 | DOI: https://doi.org/10.1524/ract.2008.1567

Abstract

Dimethyl 2-(fluoromethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 4a, a fluorinated nifedipine analog, has been shown to elicit significant calcium channel blocker activity using a guinea pig ileal longitudinal smooth muscle model. In order to perform biological studies for detection of L-type calcium channel distribution, we decided to prepare the [ 18F]-labeled compound. The latter compound was prepared in no-carrier-added (n.c.a.) form from dimethyl 2-(bromomethyl)-6-methyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate 2 in one step at 80 °C in Kryptofix[222]/K[ 18F]F and acetonitrile as a solvent in 15 min. Column chromatography afforded the radiochemically pure compound in 20 min. Radiochemical purity of the 18F-nifedipine was determined by RTLC and HPLC (>98%) and specific activity of 21–48 GBq/μmol (EOB).

Keywords: Fluorine-18; Dihydropyridines; Fluorination; Radiopharmaceutical; Nifedipine

About the article

* Correspondence address: Nuclear Medicine Research Group, Agricultural,, Medical and Industrial Research School (AMIRS), P.O. Box 31485-4395, Karaj, Iran,


Published Online: 2009-09-25

Published in Print: 2008-12-01


Citation Information: Radiochimica Acta, Volume 96, Issue 12, Pages 849–854, ISSN (Online) 2193-3405, ISSN (Print) 0033-8230, DOI: https://doi.org/10.1524/ract.2008.1567.

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