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首页> 外文期刊>Journal of Cerebral Blood Flow and Metabolism: Official Journal of the International Society of Cerebral Blood Flow and Metabolism >Evaluation of [F-18]MC225 as a PET radiotracer for measuring P-glycoprotein function at the blood-brain barrier in rats: Kinetics, metabolism, and selectivity
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Evaluation of [F-18]MC225 as a PET radiotracer for measuring P-glycoprotein function at the blood-brain barrier in rats: Kinetics, metabolism, and selectivity

机译：评估[F-18] MC225作为宠物放射反射仪，用于测量大鼠血脑屏障的P-糖蛋白功能：动力学，新陈代谢和选择性

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P-glycoprotein is a protective efflux transporter at the blood-brain barrier showing altered function in many neurological disorders. The purpose of this study was to validate [F-18]MC225 as a radiotracer for measuring P-glycoprotein function with positron emission tomography. Three groups of Sprague-Dawley rats were used to assess tracer uptake at baseline (group 1), after inhibition of P-glycoprotein (group 2), and after inhibition of both P-glycoprotein and breast cancer resistance protein (Bcrp, group 3). A two-tissue compartment model with a metabolite-corrected plasma input function provided the best fit to the positron emission tomography data, but parameter estimates were more reliable in a one-tissue compartment model, which was selected as the preferred model. Regional distribution volumes (V-T) in the control group ranged from 6 to 11, which is higher than for other radiotracers. [F-18]MC225 showed transporter selectivity, since inhibition of P-glycoprotein caused a two to fourfold increase in the cerebral V-T values, but additional inhibition of Bcrp did not cause any further increase. Metabolic stability of [F-18]MC225 was moderate (at 1h post-injection 15% of plasma radioactivity and 76% of brain radioactivity represented intact parent). Thus, [F-18]MC225 may be a useful radiotracer to measure especially increases of P-glycoprotein function at the blood-brain barrier.
机译：p-糖蛋白是血脑屏障的保护性外流转运蛋白，显示许多神经系统疾病中的功能改变。本研究的目的是将[F-18] MC225验证为用于测量具有正电子发射断层扫描的p-糖蛋白功能的放射反射液。三组Sprague-Dawley大鼠用于评估基线（第1组），抑制p-糖蛋白（第2组），以及抑制p-糖蛋白和乳腺癌抗性蛋白（BCRP，第3组）后的基线（第1组）。 。具有代谢物校正的等离子体输入功能的双组织隔间模型，提供了最适合的正电子发射断层扫描数据，但是参数估计在一个组织隔室模型中更可靠，选择作为优选模型。对照组的区域分布量（V-T）范围为6至11，高于其他放射体制粉机。 [F-18] MC225显示转运蛋白选择性，因为抑制p-糖蛋白引起脑V-T值中的两个至四倍，但对BCRP的额外抑制不会导致进一步增加。 [F-18] MC225的代谢稳定性适度（在注射后1H后血浆放射性的15％，76％的脑放射性表示完整的父母）。因此，[F-18] MC225可以是有用的辐射酸酯，以测量血脑屏障在血脑屏障下的p-糖蛋白功能的尤其增加。

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