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J Nucl Med. 2008; 49 (Supplement 1):286P
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Radiopharmaceutical Chemistry: New Chemistry-Neurosciences

New Chemistry-Neurosciences Posters

Radiosynthesis of the mGluR2/3 PET tracer (S,S,S)-2-(2-carboxycyclopropyl)-2-(4-[11C]methoxyphenethyl)glycine dimethyl ester ([11C]CMG)

Ji-Quan Wang1, Darshini Kuruppu1 and Anna-Liisa Brownell1

1 Radiology, Massachusetts General Hospital, Boston, Massachusetts

1222

Objectives: Metabotropic glutamate receptors (mGluRs) have a major role in several neurological/psychiatric disorders. Here we intend to synthesize a specific PET ligand for in vivo imaging of mGluR2/3.

Methods: [11C]CH3I was bubbled at room temperature (RT) through a mixture of the precursor (S,S,S)-N-(tert-butoxycarbonyl)-2-(2-carboxycyclopropyl)-2-(4-hydroxyphenethyl)glycine dimethyl ester (2.7 mg), K2CO3 (2 µl, 9%) and DMSO (0.4 ml). After activity trapping the mixture was heated at 120°C for 7 min. After brief cooling the mixture was injected into HPLC with solvent. The radiolabeled intermediate was isolated. After HPLC solvent removal in vacuo, trifluoroacetic acid (TFA, 0.2 ml) in CH2Cl2 (3 ml) was added to the residue. The solution was rotated for 3 min at RT. K2CO3 aqueous solution (1.5 ml, 14%) was cautiously added to quench the reaction. CH2Cl2 was removed by vacuum, and HPLC solvent (1 ml) was added. The resulted mixture was injected into HPLC and [11C]CMG was collected. 0.4-0.5 mCi of [11C]CMG was administered into the anesthetized (isoflurane) rats (male Spraque Dawley) in a microPET scanner. Dynamic volumetric data were acquired in 6 rats for 60 min.

Results: [11C]CMG was synthesized manually. Due to the limitation of our facility, only 1.5 mCi of final product was obtained after the 90 minute synthesis. Fast reversible binding was observed in several cortical areas, hippocampus, striatum and olfactory bulb. The maximum binding (1.1-1.6% of the injected dose per cm3) was observed 2 min after administration.

Conclusions: [11C]CMG was synthesized successfully and it binds into the brain areas, which have shown in immunohistochemical analysis to express mGluR2/3 receptors. This is the first in vivo PET tracer for mGluR2/3.

Research Support: NIH-NIBIB EB001850





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Right arrow Articles by Wang, J.-Q.
Right arrow Articles by Brownell, A.-L.