首页> 外文期刊>Life sciences >ROUTES OF ADMINISTRATION AND EFFECT OF CARBIDOPA PRETREATMENT ON 6-[F-18]FLUORO-L-DOPA/PET SCANS IN NON-HUMAN PRIMATES
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ROUTES OF ADMINISTRATION AND EFFECT OF CARBIDOPA PRETREATMENT ON 6-[F-18]FLUORO-L-DOPA/PET SCANS IN NON-HUMAN PRIMATES

机译:卡比多巴预处理对非人源6- [F-18] Fluoro-L-DOPA / PET领域的管理和效果

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In 6-[F-18]fluoro-L-dopa (Fdopa)/positron emission tomography (PET) studies, carbidopa pretreatment increases the Fdopa bioavailability to the brain and enhances the intensity of striatal PET images. Different PET research teams have used various carbidopa doses and routes of administration in non-human primate studies. The purpose of this study was to examine the plasma profiles of carbidopa and the effect of the route of administration of carbidopa on a Fdopa/PET scan. Cynomolgus monkeys were given carbidopa either orally (5 mg/kg), intraperitoneally (2.5 and 5 mg/kg) or intravenously (5 mg/kg) 60-90 min prior to the Fdopa injection. Carbidopa-treated monkeys were compared to monkeys without carbidopa treatment. No carbidopa was detected in the plasma samples when it was given orally, possibly due to poor absorption in the gastrointestinal tract. In addition, the striatal and cortical activities were not statistically different from those of the untreated monkeys, indicating that little or no inhibition of the peripheral decarboxylation of Fdopa by carbidopa had taken place. When carbidopa was given intraperitoneally at a dose of 2.5 and 5 mg/kg and intravenously at 5 mg/kg, plasma carbidopa concentrations at the time of Fdopa injection were 0.95 +/- 0.26, 2.22 +/- 0.23 and 2.79 +/- 0.26 mu g/ml, respectively. Because of inhibition of peripheral decarboxylation of Fdopa by carbidopa, more Fdopa was available for transport into the brain and as a result, both the striatal and cortical activities were significantly higher than those of the untreated monkeys, Carbidopa administration had no effect on either the striatal-to-cortical activity ratio or the striatum uptake value. [References: 18]
机译:在6- [F-18]氟-L-多巴(Fdopa)/正电子发射断层扫描(PET)研究中,卡比多巴预处理可提高Fdopa对大脑的生物利用度并增强纹状体PET图像的强度。不同的PET研究团队在非人类灵长类动物研究中使用了各种卡比多巴剂量和给药途径。这项研究的目的是检查卡比多巴的血浆特征以及卡比多巴给药途径对Fdopa / PET扫描的影响。在食入Fdopa前60-90分钟,给食蟹猴口服卡比多巴(5 mg / kg),腹膜内(2.5和5 mg / kg)或静脉内(5 mg / kg)。将用卡比多巴处理的猴子与未用卡比多巴处理的猴子进行比较。口服血浆样品中未发现卡比多巴,可能是由于胃肠道吸收不良所致。另外,纹状体和皮质活性与未处理的猴子没有统计学差异,表明卡比多巴对Fdopa周边脱羧的抑制作用很小或没有。当腹膜内给予卡比多巴的剂量为2.5和5 mg / kg,静脉内给予5 mg / kg时,注射Fdopa时血浆卡比多巴的浓度为0.95 +/- 0.26、2.22 +/- 0.23和2.79 +/- 0.26 μg / ml。由于卡比多巴抑制了Fdopa的外周脱羧,因此有更多的Fdopa可转运到大脑,因此纹状体和皮质活性均显着高于未处理的猴子,Carbidopa给药对纹状体均无影响-皮质活性比或纹状体摄取值。 [参考:18]

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