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标题：ACIDIC DRUG TRANSPORT IN VIVO THROUGH THE BLOOD-BRAIN BARRIER. A ROLE OF THE TRANSPORT CARRIER FOR MONOCARBOXYLIC ACIDS
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作者：Young KANG ; Tetsuya TERASAKI ; Akira TSUJI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1990
卷号：13
期号：2
页码：158-163
DOI：10.1248/bpb1978.13.158
出版社：The Pharmaceutical Society of Japan
摘要：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 [¹⁴C] 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 [¹⁴C] 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 [¹⁴C] salicylic acid. Similar results were obtained in the BBB uptake of [¹⁴C] 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.
关键词：brain uptake index