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논문 기본 정보
- 자료유형
- 학술대회자료
- 저자정보
- 저널정보
- 한국응용약물학회 한국응용약물학회 추계학술발표논문집 한국응용약물학회 2003년도 Annual Meeting of KSAP : International Symposium on Pharmaceutical and Biomedical Sciences on Obesity
- 발행연도
- 2003.1
- 수록면
- 106 - 106 (1page)
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Choline serves critical roles in the CNS both as a precursor of neurotransmitter and as an essential component of membrane phospholipids. The long-term maintenance of brain choline concentration is dependent on choline transport across the blood-brain barrier (BBB), And, we examined to elucidate the characteristics of transport of choline across the BBB using conditionally immortalized rat brain capillary endothelial cell line (TR-BBB) in vitro. The ［$^3$H］choline in TR - BBB was increased by time dependently, but independent on Na$\^$＋/, and the transport process is saturable with Michaelis-Menten constrant, Km of about 26 ${\mu}$M. The uptake of ［$^3$H］choline is susceptible for inhibition by various organic cationic compounds including hemicholinium-3, tetraethylammonium chloride (TEA) and $\ell$-carnitine. Also, we investigated the relationship of transport of choline and cationic drugs. The uptake of ［$^3$H］choline is inhibited by antioxidant, a-phenyl-n-tert-butyl nitrone (PBN) with IC$\sub$50/ of 1.2 mM. and by Alzheimer's disease therapeutics, such as acetyl $\ell$-carnitine, tacrine and donepezil. Also, choline uptake presented competitive inhibition with PBN, donepezil and acetyl $\ell$-carnitine in Lineweaver-Burk plot. In conclusion, TR-BBB cells express a saturable transport system for uptake of choline, and several cationic drugs may be transported into the brain by BBB choline transporter.
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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)
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Characterization of choline transport in immortalized rat brain capillary endothleial cell lines (TR-BBB)
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Blood-Brain Barrier Interfaces and Brain Tumors
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Targeting of Large-molecule Radiopharmaceuticals across the Blood-brain Barrier Using Endogenous Transport Systems
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