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首页> 外文期刊>Neuroscience Letters: An International Multidisciplinary Journal Devoted to the Rapid Publication of Basic Research in the Brain Sciences >1-Benzyl-1,2,3,4-tetrahydroisoquinoline passes through the blood-brain barrier of rat brain: an in vivo microdialysis study.
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1-Benzyl-1,2,3,4-tetrahydroisoquinoline passes through the blood-brain barrier of rat brain: an in vivo microdialysis study.

机译：1-苄基1,2,3,4-四氢异喹啉穿过大鼠脑的血脑屏障：一项体内微透析研究。

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摘要

Previous work has established that 1-benzyl-1,2,3,4-tetrahydroisoquinoline (1-BnTIQ) causes a parkinsonian syndrome in rats. The present study reports the blood-brain barrier (BBB) permeability of 1-BnTIQ in freely moving rats with the aid of in vivo microdialysis-based measurements. The microdialysis probe was implanted in the frontal cortex of rat brain. Brain dialysate samples were analyzed using an HPLC-MS/MS assay. 1-BnTIQ, when administered i.p., dose-dependently appeared in brain extracellular fluid (ECF), reaching a maximum concentration after about 40 min. Two other tetrahydroisoquinoline derivatives, 1,2,3,4-tetrahydroisoquinoline (TIQ) and 6,7-dihydroxy-1-methyl-1,2,3,4-tetrahydroisoquinoline [salsolinol (SAL)], served as positive and negative controls, respectively. The results confirmed an earlier report that SAL does not reach the brain after i.p. administration. In contrast, TIQ readily passed through the BBB. The brain dialysate concentration of 1-BnTIQ was about 24% that of TIQ when administered i.p. at the same dose. Both of them decreased quickly with a half-life of about 50 min.
机译：先前的工作已确定1-苄基-1,2,3,4-四氢异喹啉（1-BnTIQ）引起大鼠帕金森氏综合征。本研究报告了在体内基于微透析的测量的帮助下，自由运动大鼠中1-BnTIQ的血脑屏障（BBB）渗透性。将微透析探针植入大鼠大脑的额叶皮层。使用HPLC-MS / MS分析法分析了脑透析液样品。腹膜内注射时1-BnTIQ剂量依赖性地出现在脑细胞外液（ECF）中，约40分钟后达到最大浓度。其他两种四氢异喹啉衍生物1,2,3,4-四氢异喹啉（TIQ）和6,7-二羟基-1-甲基-1,2,3,4-四氢异喹啉[salsolinol（SAL）]用作阳性和阴性对照， 分别。该结果证实了较早的报道，即SAL在i.p.后未到达大脑。行政。相反，TIQ轻松通过了BBB。腹膜内注射时，1-BnTIQ的脑透析液浓度约为TIQ的24％。以相同的剂量。两者均迅速下降，其半衰期约为50分钟。

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