A Convenient Radiolabeling of 11C(R)-PK11195 Using Loop Method in Automatic Synthesis Module / 핵의학분자영상
Nuclear Medicine and Molecular Imaging
;
: 337-343, 2009.
Artigo
em Coreano
| WPRIM
| ID: wpr-33864
ABSTRACT
PURPOSE:
((R)-1-(2-chlorophenyl)-N-1-[11C]methyl-N-(1-propyl)-3-isoquinoline carboxamide ((R)-PK11195) is a specific ligand for the peripheral type benzodiazepine receptor and a marker of activated microglia, used to measure inflammation in neurologic disorders. We report here that a direct and simple radiosynthesis of [11C](R)-PK11195 inmild condition using NaH suspension in DMF and one-step loop method. MATERIALS ANDMETHODS:
(R)-NDesmethyl- PK11195 (1 mg) in DMSO (0.1 mL) and NaH suspension in DMF (0.1 mL) were injected into a semi-prep HPLC loop. [11C]methyl iodide was passed through HPLC loop at room temperature. Purification was performed using semi-preparative HPLC. Aliquots eluted at 11.3 min were collected and analyzed by analytical HPLC and mass spectrometer.RESULTS:
The labeling efficiency of [11C](R)-PK11195 was 71.8+/-8.5%. The specific activity was 11.8 +/-6.4 GBq/micromol and radiochemical purity was higher than 99.2%. The mass spectrum of the product eluted at 11.3 min showed m/z peaks at 353.1 (M+1), indicating the mass and structure of (R)-PK11195.CONCLUSION:
By the one-step loop method with the [11C]CH3I automated synthesis module, [11C](R)-PK11195 could be easily prepared in high radiochemical yield using NaH suspension in DMF.
Texto completo:
DisponíveL
Índice:
WPRIM (Pacífico Ocidental)
Assunto principal:
Dimetil Sulfóxido
/
Cromatografia Líquida de Alta Pressão
/
Microglia
/
Receptores de GABA-A
/
Inflamação
/
Isoquinolinas
/
Doenças do Sistema Nervoso
Idioma:
Coreano
Revista:
Nuclear Medicine and Molecular Imaging
Ano de publicação:
2009
Tipo de documento:
Artigo
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