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학술연구/단체지원/교육 등 연구자 활동을 지속하도록 DBpia가 지원하고 있어요.
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논문 기본 정보
- 자료유형
- 학술저널
- 저자정보
- 발행연도
- 2019.1
- 수록면
- 290 - 301 (12page)
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초록· 키워드
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Paeonol has neuroprotective function, which could be useful for improving central nervous system disorder. The purpose of this study was to characterize the functional mechanism involved in brain transport of paeonol through blood-brain barrier (BBB). Brain transport of paeonol was characterized by internal carotid artery perfusion (ICAP), carotid artery single injection technique (brain uptake index, BUI) and intravenous (IV) injection technique in vivo. The transport mechanism of paeonol was examined using conditionally immortalized rat brain capillary endothelial cell line (TR-BBB) as an in vitro model of BBB. Brain volume of distribution (VD) of [$^3H$]paeonol in rat brain was about 6-fold higher than that of [$^{14}C$]sucrose, the vascular space marker of BBB. The uptake of [$^3H$]paeonol was concentration-dependent. Brain volume of distribution of paeonol and BUI as in vivo and inhibition of analog as in vitro studies presented significant reduction effect in the presence of unlabeled lipophilic compounds such as paeonol, imperatorin, diphenhydramine, pyrilamine, tramadol and ALC during the uptake of [$^3H$]paeonol. In addition, the uptake significantly decreased and increased at the acidic and alkaline pH in both extracellular and intracellular study, respectively. In the presence of metabolic inhibitor, the uptake reduced significantly but not affected by sodium free or membrane potential disruption. Similarly, paeonol uptake was not affected on OCTN2 or rPMAT siRNA transfection BBB cells. Interestingly. Paeonol is actively transported from the blood to brain across the BBB by a carrier mediated transporter system.
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등록된 정보가 없습니다.
참고문헌 (55)
참고문헌 신청
Abbott NJ / 2010 / Structure and function of the blood-brain barrier / Neurobiol. Dis 37:13~25
Andre P / 2009 / Clonidine transport at the mouse blood-brain barrier by a new H+ antiporter that interacts with addictive drugs / J. Cereb. Blood Flow Metab 29:1293~1304
Bickel U / 1996 / Poor permeability of morphine 3-glucuronide and morphine 6-glucuronic through the blood-brain barrier in the rat / J. Pharmacol. Exp. Ther 278:107~113
Boström E / 2006 / In vivo blood-brain barrier transport of oxycodone in the rat : indications for active influx and implications for pharmacokinetics/pharmacodynamics / Drug Metab. Dispos 34:1624~1631
Chapy H / 2014 / Carrier-mediated cocaine transport at the blood-brain barrier as a putative mechanism in addiction liability / Int. J. Neuropsychopharmacol 18:1~10
Andre P / 2009 / Clonidine transport at the mouse blood-brain barrier by a new H+ antiporter that interacts with addictive drugs / J. Cereb. Blood Flow Metab 29:1293~1304
Bickel U / 1996 / Poor permeability of morphine 3-glucuronide and morphine 6-glucuronic through the blood-brain barrier in the rat / J. Pharmacol. Exp. Ther 278:107~113
Boström E / 2006 / In vivo blood-brain barrier transport of oxycodone in the rat : indications for active influx and implications for pharmacokinetics/pharmacodynamics / Drug Metab. Dispos 34:1624~1631
Chapy H / 2014 / Carrier-mediated cocaine transport at the blood-brain barrier as a putative mechanism in addiction liability / Int. J. Neuropsychopharmacol 18:1~10
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