The efflux transport of choline through blood-brain barrier is inhibited by Alzheimer's disease therapeutics

Abstract

In the present study, we examined the effects of several therapeutics of Alzheimer's disease, such as donepezil hydrochloride, tacrine and α-phenyl-n-tert-butyl nitrone (PBN) on choline efflux from brain to circulating blood. The brain-to-blood efflux of [3H]choline in rats was significantly inhibited by tacrine and PBN. Also the [3H]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.