Radiosynthesis of peripheral benzodiazepine receptor radioligand N-methyl-(11)CPK 11195 as an imaging agent for positron emission tomography / 南方医科大学学报
Journal of Southern Medical University
; (12): 2425-2428, 2009.
Article
em Zh
| WPRIM
| ID: wpr-325099
Biblioteca responsável:
WPRO
ABSTRACT
<p><b>OBJECTIVE</b>To establish a protocol of automated synthesis of 1-(2-chlorophenyl)-N-[(11)C]methyl-N-(1-methylpropyl)-3-isoquinoline carboxamide ((11)C-PK11195) as the positron-emitter-labeled ligand for peripheral benzodiazepine receptor (PBR) using a commercial synthesizer and explore the quality control methods for the resulting product.</p><p><b>METHODS</b>(11)C-methyl iodide ((11)C-CH(3)I) was synthesized via liquid-phase distillation approach using a (11)C-iodomethane synthesizer. (11)C-PK11195 was prepared by (11)C-methylation of 1-(2-chlorophenyl)-N-(1-methylpropyl)-3-isoquinoline carboxamide (N-demethyl-PK 11195) as the precursor with (11)C-CH(3)I and purified by semi-preparative reversed phase high performance liquid chromatography (HPLC). The radiochemical purity, chemical purity and stability of the product were evaluated by HPLC, and the toxicity was assessed in normal mice. The factors that affected (11)C-PK11195 synthesis were also studied.</p><p><b>RESULTS</b>(11)C-PK11195 was successfully synthesized using the TracerLab FX(F-N) synthesizer. The synthesis time was about 35 min from the end of (11)C-carbon dioxide production by cyclotron to the end of (11)C-PK11195 synthesis (EOS), with a (11)C-methylation reaction time of 3-4 min. The uncorrected radiochemical yield for (11)C-methylation was (33-/+5)%. Analysis with radio-analytical HPLC showed a radiochemical purity and chemical purity of the product both exceeding 99%, with a specific radioactivity of 30-65 GBq/micromol at EOS (from the end of radionuclide production). The (11)C-PK11195 synthesized was radiochemically stable at room temperature and showed low toxicity in normal mice.</p><p><b>CONCLUSION</b>The (11)C-PK11195 injection can be conveniently prepared using an automated synthesizer for clinical use in positron emission tomography.</p>
Texto completo:
1
Índice:
WPRIM
Assunto principal:
Ensaio Radioligante
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Radioisótopos de Carbono
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Receptores de GABA-A
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Meios de Contraste
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Compostos Radiofarmacêuticos
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Tomografia por Emissão de Pósitrons
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Isoquinolinas
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Metabolismo
Tipo de estudo:
Guideline
Limite:
Animals
Idioma:
Zh
Revista:
Journal of Southern Medical University
Ano de publicação:
2009
Tipo de documento:
Article