ACIDIC DRUG TRANSPORT IN VIVO THROUGH THE BLOOD-BRAIN BARRIER. A ROLE OF THE TRANSPORT CARRIER FOR MONOCARBOXYLIC ACIDS
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概要
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The relationship of the transports between acidic drugs and monocarboxylic acids through the blood-brain barrier (BBB) was examined using the carotid artery injection technique in rats. The BBB uptakes of [^3H] acetic acid and [^<14>C] salicylic acid were significantly reduced by the presence of the respective unlabeled compounds, valproic acid, lactic acid, benzoic acid, nicotinic acid or β-lactam antibiotics (benzylpenicillin, propicillin and cefazolin), but was not reduced by choline, phenylalanine and a basic drug, eperisone. A remarkable pH dependency was observed for the BBB uptake of [^<14>C] salicylic acid at the pH region of 4.0 to 7.4. Interestingly, 10 mM of salicylic acid diminished significantly the pH dependent BBB uptake of [^<14>C] salicylic acid. Similar results were obtained in the BBB uptake of [^<14>C] nicotinic acid. No significant difference was observed in the transport of monocarboxylic acids through the BBB between normotensive Wistar KY rats (WKY) and stroke-prone spontaneously hypertensive rats (SHRSP). From these observations, acidic drugs could be transported by a carrier-mediated system for monocarboxylic acids at the BBB and the transport system was not changed by the disease state.
- 公益社団法人日本薬学会の論文
著者
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Tsuji Akira
Faculty Of Pharmaceutical Sciences Kanazawa University
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Tsuji Akira
金沢大学 薬
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Tsuji Akira
富山化学工業綜合研究所
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TERASAKI Tetsuya
Faculty of Pharmaceutical Sciences, Kanazawa University
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Tsuji A
Kanazawa Univ. Ishikawa Jpn
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Kang Youngsook
Faculty Of Pharmaceutical Sciences Kanazawa University
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Kang Young
Faculty Of Pharmaceutical Sciences Kanazawa University
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Tsuji Akira
Department Of Pediatrics:hospital Pharmacy:and Faculty Of Pharmaceutical Sciences University Of Kana
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Terasaki Tetsuya
Faculty Of Pharmaceutical Sciences Kanazawa University
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Terasaki Tetsuya
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Kanazawa University
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Kang Young
Faculty Of Mechanical And Aerospace System Eng. Chonbuk National Univ.
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Terasaki T
Kanazawa Univ. Kanazawa Jpn
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