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J Nucl Med. 2008; 49 (Supplement 1):288P
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Radiopharmaceutical Chemistry: New Chemistry-Neurosciences

New Chemistry-Neurosciences Posters

Radiosynthesis of (±)-N-(p-[11C]tolyl)-7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxamide ([11C]methyl-PHCCC) as a specific mGluR4 PET ligand

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

1 Radiology, Massachusetts General Hospital, Boston, Massachusetts

1231

Objectives: Metabotropic glutamate receptors (mGluRs) have a major role in signal transmission in the brain. We aim to synthesize a PET ligand for imaging of mGluR4 in different neurological conditions.

Methods: Dry DMF (0.4 ml) was added to a V-vial previously flushed with argon and charged with tris(dibenzylideneacetone)dipalladium (1.4 mg) and tri(o-tolyl)phosphine (2.0 mg). [11C]Methyl iodide was bubbled through the solution and trapped for 3 min. After this dry DMF (0.6 ml) was freshly added to a second V-vial previously flushed with argon containing the precursor (±)-N-(p-trimethylstannylphenyl)-7-(hydroxyimino)cyclopropa [b]chromen-1a-carboxamide (1.7 mg), copper (I) chloride (1.1 mg) and potassium carbonate (0.8 mg). The activity was transferred to the second V-vial, vortexed for half min and heated at 80°C for 8 min. After cooling for 1 min HPLC solvent (1 ml) was added to the reaction vial, and the mixture was filtered with 50 µm filter. The filtrate was injected into a semi-preparative HPLC and eluted with a mixture of methanol (70%) and water (30%). Using flow rate of 4 ml/min, the pure compound came at 5-6 min. The ligand was tested in 4 normal and 2 Parkinson’s disease (PD) rat models.

Results: Total activity after 60 min synthesis and HPLC purification was 76 mCi with purity ≥97%. In the PET studies fast accumulation (max at 3-6 min) of the radioactivity was observed in several brain areas including cortical areas (SC), striatum, thalamus, hypothalamus, subthalamic nucleus (STN), olfactory area. In the PD rats we observed moderately enhanced accumulation in the STN and spinal cord.

Conclusions: [11C]Methyl-PHCCC was synthesized successfully. These preliminary studies indicate that the mGluR4 receptors might have a role in the PD-like degeneration.

Research Support: NIH-NIBIB EB001850





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Right arrow Articles by Brownell, A.-L.