Huang S C, Stout D B, Yee R E, Satyamurthy N, Barrio J R
Department of Molecular and Medical Pharmacology, and Laboratory of Structural Biology and Molecular Medicine (DOE), UCLA School of Medicine, Los Angeles, California 90095-6948, USA.
J Cereb Blood Flow Metab. 1998 Dec;18(12):1288-93. doi: 10.1097/00004647-199812000-00002.
Variations in the cerebellum to plasma ratio at late times in 6-[18F]fluoro-L-DOPA studies are shown to be consistent with competitive binding of large neutral amino acids for a common transporter in the blood-brain barrier and the stability of brain tissue large neutral amino acid level in the presence of plasma level changes. The distribution volume of an inert large neutral amino acid can be estimated from plasma and tissue large neutral amino acid levels and apparent half-saturation concentrations (Km) of the transporter in the blood-brain barrier. Stability of brain large neutral amino acid levels is supported by literature findings and can be explained by high saturation of the large neutral amino acid transporter at physiologic conditions.
在6-[¹⁸F]氟-L-多巴研究的后期,小脑与血浆比值的变化表明,这与血液-脑屏障中共同转运体对大中性氨基酸的竞争性结合以及血浆水平变化时脑组织大中性氨基酸水平的稳定性一致。惰性大中性氨基酸的分布容积可根据血浆和脑组织大中性氨基酸水平以及血液-脑屏障中转运体的表观半饱和浓度(Km)来估算。脑组织大中性氨基酸水平的稳定性得到了文献研究结果的支持,并且可以通过生理条件下大中性氨基酸转运体的高饱和度来解释。