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Updated: May 23, 2026

A Simple and Reproducible Method to Prepare Membrane Samples from Freshly Isolated Rat Brain Microvessels
Published on: May 7, 2018
The blood-brain barrier choline transporter
Werner J Geldenhuys1, David D Allen
1Department of Pharmaceutical Sciences, Northeast Ohio Medical University, 4209 State Route 44, Rootstown, OH 44272, USA. wgeldenh@neomed.edu
Designing brain-penetrating drugs requires understanding the blood-brain barrier (BBB). This review details structural needs for organic cation transporters (OCTs) to improve central nervous system (CNS) drug delivery.
Area of Science:
- Neuroscience
- Pharmacology
- Biochemistry
Background:
- The blood-brain barrier (BBB) restricts drug entry into the central nervous system (CNS).
- Specific transporters in the BBB vasculature offer potential routes for drug delivery.
- Organic cation transporters (OCTs) are key targets for delivering cationic compounds to the CNS.
Purpose of the Study:
- To review structural requirements for designing compounds that utilize organic cation transporters (OCTs) for brain drug delivery.
- To compare the structural needs for OCT1, OCT2, and the BBB choline transporter (BBBCHT).
Main Methods:
- Literature review of existing research on organic cation transporters and BBB transport.
- Comparative analysis of structural features influencing substrate recognition by OCT1, OCT2, and BBBCHT.
Main Results:
- Identified key structural determinants for OCT1 and OCT2 substrate binding.
- Compared these determinants with those of the BBB choline transporter (BBBCHT).
- Highlighted differences and similarities in transporter specificity.
Conclusions:
- Understanding structural requirements for OCTs can guide the design of CNS-penetrant drugs.
- This knowledge can enhance the efficacy of drug delivery across the BBB.
- Potential for improved therapeutic outcomes in CNS disorders.
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16:26Setting-up an In Vitro Model of Rat Blood-brain Barrier (BBB): A Focus on BBB Impermeability and Receptor-mediated Transport
Published on: June 28, 2014
10:30High-resolution Confocal Imaging of the Blood-brain Barrier: Imaging, 3D Reconstruction, and Quantification of Transcytosis
Published on: November 16, 2017
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