RESUMEN
INTRODUCTION: Carbon-11-labeled phosgene is an important labeling precursor for PET molecular probes. Despite the usefulness of [(11)C]phosgene, some difficulties, especially in the formation of [(11)C]phosgene process from [(11)C]CCl(4), hamper its use. The present article shows a simple preparation method for [(11)C]phosgene. METHOD: [(11)C]CCl(4) was obtained using the conventional method by passing a mixture of [(11)C]CH(4) and Cl(2) through a heated quartz tube. The [(11)C]CCl(4) was transformed to [(11)C]phosgene simply by passing through a pretreatment tube of a Kitagawa gas detection system for the working-environmental CCl(4) concentration measurement at room temperature with a flow rate of 50 ml/min. RESULT: This tube successfully transformed [(11)C]CCl(4) to [(11)C]phosgene at room temperature. [(11)C]Phosgene was obtained at nearly 80% radiochemical yield (EOB) in a short synthesis time with high reproducibility. CONCLUSION: A high yield and reliable [(11)C]phosgene production method using a gas detector tube system for working-environmental CCl(4) concentration measurement was developed.
Asunto(s)
Tetracloruro de Carbono/análisis , Tetracloruro de Carbono/química , Gases/análisis , Gases/química , Fosgeno/química , Fosgeno/síntesis química , Radioisótopos de Carbono/química , Tetracloruro de Carbono/síntesis química , Gases/síntesis química , Reproducibilidad de los Resultados , TemperaturaRESUMEN
Se examinó el extracto acuoso y etanólico (100 mg/kg) de Luffa acutangula Linn (frutos) para determinar la actividadantihepatotóxica en ratas druckrey mediante la hepatotoxicidad inducida por tetracloruro de carbono (CCl4)y paracetamol (PCM). Se demostró que el extracto posee un efecto hepatoprotector signifi cativo, ya que reduce losniveles séricos de transaminasas (SGPT y SGOT), fosfatasa alcalina (ALP) y bilirrubina. La signifi cativa actividadhepatoprotectora de Luffa acutangula es comparable a la de la silimarina, agente hepatoprotector estándar, lo quejustifi ca su uso en afecciones del hígado
The ethanolic and aqueous extract (100mg/kg) of Luffa acutangula Linn(fruits) was examined for antihepatotoxic activityin druckrey rats by inducing hepatotoxicity with Carbon tetrachloride(CCl4) and Paracetamol(PCM). The extracthas shown to posses signifi cant hepatoprotective effect by lowering the serum level of transaminases (SGPT & SGOT),Alkaline phosphatase (ALP) and bilirubin. The signifi cant hepatoprotective activity of Luffa acutangula is comparableto that standard hepatoprotective agent silymarin, which justify its use in liver affection
Asunto(s)
Ratas , Masculino , Femenino , Animales , Extractos Vegetales/química , Luffa acutangula/análisis , Luffa acutangula/farmacología , Luffa acutangula/uso terapéutico , Tetracloruro de Carbono/química , Tetracloruro de Carbono/síntesis química , Acetaminofén/química , Acetaminofén/farmacología , Silimarina/farmacología , Fitoterapia/clasificación , Fitoterapia , Luffa acutangula/provisión & distribución , Tetracloruro de Carbono/análisis , Tetracloruro de Carbono/farmacología , Tetracloruro de Carbono/farmacocinética , Silimarina/farmacocinéticaAsunto(s)
Tetracloruro de Carbono/toxicidad , Carcinógenos/toxicidad , Animales , Tetracloruro de Carbono/síntesis química , Tetracloruro de Carbono/química , Tetracloruro de Carbono/farmacología , Intoxicación por Tetracloruro de Carbono/etiología , Pruebas de Carcinogenicidad , Carcinógenos/síntesis química , Carcinógenos/química , Carcinógenos/farmacología , Exposición a Riesgos Ambientales/efectos adversos , Exposición a Riesgos Ambientales/legislación & jurisprudencia , Femenino , Regulación Gubernamental , Guías como Asunto , Humanos , Masculino , Ratones , Modelos Biológicos , Ratas , Estados UnidosRESUMEN
[11C]Phosgene ([11C]COCl2), a useful precursor for labeling several radiopharmaceuticals, is generally produced by catalytic oxidation of [11C]carbon tetrachloride over Fe granules, although in low yields or with poor reproducibility. In order to develop am improved synthesis of [11C]phosgene, two oxidizing agents, Fe2O3 and CuO, were examined. The yield of [11C]phosgene was significantly increased using Fe2O3 powder mixed with Fe granules, while the use of CuO alone, or CuO powder mixed with Fe granules resulted in an insignificant yield. The yield and specific activity of S- (-) [11C]CGP-12177 synthesized using Fe2O3 powder mixed with Fe granules were markedly higher than those synthesized by the previous methods using Fe granules alone or Fe granules mixed with Fe powder. Thus, in the present study, we developed a simple and practical method for the synthesis of [11C]phosgene, which provided an improved yield of S- (-) [11C]CGP-12177.
Asunto(s)
Compuestos Ferrosos/química , Hierro/química , Fosgeno/síntesis química , Radiofármacos/síntesis química , Carbanilidas/síntesis química , Radioisótopos de Carbono , Tetracloruro de Carbono/síntesis química , Cobre/química , Marcaje Isotópico , Fosgeno/química , Propanolaminas/síntesis química , Radiofármacos/químicaRESUMEN
2-[11C]Thymidine has been produced from [11C]methane via [11C]phosgene and [11C]urea. Anhydrous [11C]urea was prepared from [11C]phosgene by reaction with liquid ammonia. This novel approach avoids the problems associated with the synthesis of anhydrous [11C]urea from [11C]cyanide. A fully automated system based on a modular approach and under PLC control has been developed. The system provides 2-[11C]thymidine reliably and reproducibly for clinical PET studies. The radiosynthesis takes 45-50 min from [11C]methane and the average yield was 1.5-3.3 GBq (40-90 mCi). The specific radioactivity was typically in the range 29.6-51.8 GBq mumol-1 (0.8-1.4 Ci mumol-1) at EOS corresponding to 6-12 micrograms of stable thymidine. The radiochemical yield of 2-[11C]thymidine was ca. 14% from [11C]methane.