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Molecules 2015, 20(6), 9550-9559;

Practical Radiosynthesis and Preclinical Neuroimaging of [11C]isradipine, a Calcium Channel Antagonist

Department of Radiology, Harvard Medical School, Division of Nuclear Medicine and Molecular Imaging and Center for Advanced Medical Imaging Sciences, Massachusetts General Hospital, 55 Fruit Street, Boston, MA 02114, USA
Department of Research, Shriners Hospitals for Children—Boston, 51 Blossom Street, Boston, MA 02114, USA
Department of Psychiatry and Center for Experimental Drugs and Diagnostics, Massachusetts General Hospital, 185 Cambridge Street, Boston, MA 02114, USA
Author to whom correspondence should be addressed.
Academic Editor: Svend Borup Jensen
Received: 28 April 2015 / Revised: 19 May 2015 / Accepted: 20 May 2015 / Published: 26 May 2015
(This article belongs to the Special Issue Preparation of Radiopharmaceuticals and Their Use in Drug Development)
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In the interest of developing in vivo positron emission tomography (PET) probes for neuroimaging of calcium channels, we have prepared a carbon-11 isotopologue of a dihydropyridine Ca2+-channel antagonist, isradipine. Desmethyl isradipine (4-(benzo[c][1,2,5]oxadiazol-4-yl)-5-(isopropoxycarbonyl)-2,6-dimethyl-1,4-dihydropyridine -3-carboxylic acid) was reacted with [11C]CH3I in the presence of tetrabutylammonium hydroxide in DMF in an HPLC injector loop to produce the radiotracer in a good yield (6 ± 3% uncorrected radiochemical yield) and high specific activity (143 ± 90 GBq·µmol−1 at end-of-synthesis). PET imaging of normal rats revealed rapid brain uptake at baseline (0.37 ± 0.08% ID/cc (percent of injected dose per cubic centimeter) at peak, 15–60 s), which was followed by fast washout. After pretreatment with isradipine (2 mg·kg−1, i.p.), whole brain radioactivity uptake was diminished by 25%–40%. This preliminary study confirms that [11C]isradipine can be synthesized routinely for research studies and is brain penetrating. Further work on Ca2+-channel radiotracer development is planned. View Full-Text
Keywords: carbon-11; radiosynthesis; isradipine; positron emission tomography; neuroimaging; calcium channel blocker carbon-11; radiosynthesis; isradipine; positron emission tomography; neuroimaging; calcium channel blocker

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Rotstein, B.H.; Liang, S.H.; Belov, V.V.; Livni, E.; Levine, D.B.; Bonab, A.A.; Papisov, M.I.; Perlis, R.H.; Vasdev, N. Practical Radiosynthesis and Preclinical Neuroimaging of [11C]isradipine, a Calcium Channel Antagonist. Molecules 2015, 20, 9550-9559.

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