The Blood-Brain Barrier Choline Transporter

Author(s): Werner J. Geldenhuys, David D. Allen

Journal Name: Central Nervous System Agents in Medicinal Chemistry
Formerly Current Medicinal Chemistry - Central Nervous System Agents

Volume 12 , Issue 2 , 2012

Become EABM
Become Reviewer


Drug delivery to the brain is made difficult by the blood-brain barrier (BBB) which is selectively permeable to organic drug compounds. Several membrane solute and nutrient transporters are expressed in the BBB vasculature, which may be utilized as mechanism of delivery of drugs to the brain. Of interest to us, are the organic cation transporters which could be used to transport cationic compounds into the CNS. In this mini-review, we will review the current understanding of the structural requirements for designing compounds which could effectively use organic cation transporters (OCT). For the first time, structural requirements for both OCT1 and OCT2 versus the BBB choline transporter (BBBCHT) are discussed and compared. The information gained here could increase the success rate in successful CNS drug delivery and therapeutics.

Keywords: In situ brain perfusion, logPS, organic cation transporters, OCT, SLC22A, donepezil, CNS permeability, blood-brain barrier (BBB)

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2012
Published on: 31 May, 2012
Page: [95 - 99]
Pages: 5
DOI: 10.2174/187152412800792670
Price: $65

Article Metrics

PDF: 44