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Updated: May 14, 2026

Reconstruction of the Blood-Brain Barrier In Vitro to Model and Therapeutically Target Neurological Disease
Published on: October 20, 2023
[Multi-disciplinary research approaches on the brain barrier transport system, a dynamic interface]
Masanori Tachikawa1, Yasuo Uchida, Tetsuya Terasaki
1Graduate School of Pharmaceutical Sciences, Tohoku University, Sendai, Japan.
Brain barriers like the blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB) utilize transporters to manage compound entry and exit. Understanding these transport systems is crucial for effective central nervous system (CNS) drug delivery.
Area of Science:
- Neuroscience
- Pharmacology
- Biochemistry
Context:
- The blood-brain barrier (BBB) and blood-cerebrospinal fluid barrier (BCSFB) are critical interfaces regulating the central nervous system (CNS) environment.
- These barriers possess complex carrier-mediated transport systems essential for brain function and protection.
- Dysfunction in these transport systems is implicated in various CNS disorders.
Purpose:
- To review current knowledge and methodologies concerning transport systems at the human brain barriers.
- To highlight the role of these transporters in the disposition of endogenous and xenobiotic compounds.
- To emphasize the significance of brain barrier transport for CNS drug delivery and therapeutic strategies.
Summary:
- Carrier-mediated transport systems at the BBB and BCSFB facilitate or restrict the passage of molecules, impacting CNS drug delivery.
- Influx transporters like LAT1/SLC7A5 aid CNS entry, while efflux transporters (e.g., P-glycoprotein, BCRP, MRP4) limit it.
- Quantitative targeted absolute proteomics (QTAP) enables precise measurement of transporter expression, aiding in the reconstruction of in vivo transport functions.
Impact:
- Provides a foundation for understanding the pathophysiological roles of brain barriers.
- Informs the development of rational drug delivery and targeting strategies for CNS therapeutics.
- Enhances knowledge of how the brain manages endogenous neurotoxic compounds and xenobiotics.
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