Lockman Paul R, McAfee James H, Geldenhuys Werner J, Allen David D
Department of Pharmaceutical Sciences, School of Pharmacy, Texas Tech University HSC, Amarillo, Texas 79106-1712, USA.
Neurochem Res. 2004 Dec;29(12):2245-50. doi: 10.1007/s11064-004-7032-4.
The molecular identification, expression and cloning of membrane-bound organic cation transporters are being completed in isolated in vitro membranes. In vivo studies, where cation specificity overlaps, need to complement this work.
Cross-inhibition of [3H]choline and [3H]thiamine brain uptake by in situ rat brain perfusion.
[3H]Choline brain uptake was not inhibited by thiamine at physiologic concentrations (100 nM). However, choline ranging from 100 nM to 250 microM inhibited [3H]thiamine brain uptake, though not below levels observed at thiamine concentrations of 100 nM.
(1) The molecular family of the blood-brain barrier (BBB) choline transporter may be elucidated in vitro by its interaction with physiologic thiamine levels, and (2) two cationic transporters at the BBB may be responsible for thiamine brain uptake.
膜结合有机阳离子转运体的分子鉴定、表达及克隆正在体外分离的膜中完成。在体内研究中,阳离子特异性存在重叠,需要对这项工作进行补充。
通过原位大鼠脑灌注对[³H]胆碱和[³H]硫胺素脑摄取进行交叉抑制。
生理浓度(100 nM)的硫胺素不抑制[³H]胆碱脑摄取。然而,100 nM至250 μM的胆碱抑制[³H]硫胺素脑摄取,但不低于硫胺素浓度为100 nM时观察到的水平。
(1)血脑屏障(BBB)胆碱转运体的分子家族可通过其与生理硫胺素水平的相互作用在体外阐明,(2)血脑屏障处的两种阳离子转运体可能负责硫胺素脑摄取。