The Blood-Brain Barrier Choline Transporter
Werner J. Geldenhuys,
David D. Allen.
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)
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