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The Efflux Transport of Choline through Blood-Brain Barrier is Inhibited by Alzheimer's Disease Therapeutics
- Authors
- Lee, Na-Young; Kang, Young-Sook
- Issue Date
- Sep-2008
- Publisher
- KOREAN SOC APPLIED PHARMACOLOGY
- Keywords
- Blood-brain barrier; Choline transport; Alzheimer's disease therapeutics; in vivo brain efflux index method; TR-BBB cells
- Citation
- BIOMOLECULES & THERAPEUTICS, v.16, no.3, pp 179 - 183
- Pages
- 5
- Journal Title
- BIOMOLECULES & THERAPEUTICS
- Volume
- 16
- Number
- 3
- Start Page
- 179
- End Page
- 183
- ISSN
- 1976-9148
2005-4483
- Abstract
- In the present study, we examined the effects of several therapeutics of Alzheimer's disease, such as donepezil hydrochloride, tacrine and alpha-phenyl-n-tert-butyl nitrone (PBN) on choline efflux from brain to circulating blood. The brain-to-blood efflux of [H-3]choline in rats was significantly inhibited by tacrine and PBN. Also the [H-3]choline efflux was reduced by tacrine and donepezil hydrochloride in the TR-BBB cells, in vitro the blood-brain barrier (BBB) model. These results suggest that these drugs may influence choline efflux transport from brain to blood and regulate the choline level in brain resulting in the increase of acetylcholine synthesis.
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