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Donepezil, tacrine and alpha-phenyl-n-tert-butyl nitrone (PBN) inhibit choline transport by conditionally immortalized rat brain capillary endothelial cell lines (TR-BBB)

Authors
Kang, YSLee, KELee, NYTerasaki, T
Issue Date
Apr-2005
Publisher
PHARMACEUTICAL SOC KOREA
Keywords
donepezil; tacrine; PBN; choline transport; organic cation transporter; blood-brain barrier; rat brain capillary endothelial cell line
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.28, no.4, pp 443 - 450
Pages
8
Journal Title
ARCHIVES OF PHARMACAL RESEARCH
Volume
28
Number
4
Start Page
443
End Page
450
URI
https://scholarworks.sookmyung.ac.kr/handle/2020.sw.sookmyung/15520
DOI
10.1007/BF02977674
ISSN
0253-6269
1976-3786
Abstract
In the present study, we have characterized the choline transport system and examined the influence of various amine drugs on the choline transporter using a conditionally immortalized rat brain capillary enotheliald cell line (TR-BBB) in vitro. The cell-to-medium (C/M) ratio of [H-3]choline in TR-131313 cells increased time-dependently. The initial uptake rate of [H-3]choline was concentration-dependent with a Michaelis-Menten value, K-m, of 26.2 +/- 2.7 mu M. The [H-3]choline uptake into TR-131313 was Na+-independent, but was membrane potential-dependent. The [H-3]choline uptake was susceptible to inhibition by hemicholinium-3, and tetraethylammonium (TEA), which are organic cation transporter substrates. Also, the uptake of [H-3]choline was competitively inhibited with K-i values of 274 mu M, 251 mu M and 180 mu M in the presence of donepezil hydrochloride, tacrine and alpha-phenyl-n-tert-butyl nitrone (PBN), respectively. These characteristics of choline transport are consistent with those of the organic cation transporter (OCT). OCT2 mRNA was expressed in TR-BBB cells, while the expression of OCT3 or choline transporter (CHT) was not detected. Accordingly, these results suggest that OCT2 is a candidate for choline transport at the BBB and may influence the BBB permeability of amine drugs.
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