消化管及び腎尿細管におけるポリカチオン型薬物の膜透過機構

スポンサーリンク

概要

• 論文の詳細を見る

• This article reviewed the transport mechanism of polycationic compounds across rat intestinal and renal cell membranes. The inside-negative diffusion potential stimulated the initial uptake of dicationic compounds into intestinal brush-border membrane vesicles, and a good correlation was observed between lipophilicity and the amount of diffusion potential-dependent transport of the dications. On the other hand, tri- and tetracationic compounds were not affected by the diffusion potential because of their much lower lipophilicity. The membrane surface potential affected to the transport of polycationic compounds, similar to monocationic compounds. Therefore it appears that the membrane surface potential plays a common role in the transport of mono- and polycationic compounds across cell membranes. On the intestinal basolateral membrane, it was found that there was a Na^+/putrescine symporter. This recognized dicationic compounds and transported them from the blood into intestinal cells. This transporter did not recognize spermine and spermidine. Furthermore, we found a novel transport system, a Na^+/spermine antiporter, on the rat renal brush-border membrane. This transporter recognized aliphatic polycation, which has more than four amino groups, and actively secreted spermine and trientine into the renal proximal tubules in vitro and in vivo. However, this transporter did not recognize trientine-copper complex. These results are useful for the prediction of the intestinal absorption and renal excretion of polyamine derivatives.

• 社団法人日本薬学会の論文
• 2002-09-01

著者

• 小林 道也

  北海道大学医学部附属病院薬剤部

• 小林 直也

  北海道大学医学部附属病院 薬剤

関連論文

• 北大病院における処方オーダリングシステム (4) : 薬剤情報提供システムの導入
• 北大病院における処方オーダリングシステム (3) : 相互作用チェック機能の導入
• 消化管及び腎尿細管におけるポリカチオン型薬物の膜透過機構
• ESI-MSは免疫抑制剤開発のスクリーニングに有用か(C・物理化学, 分析化学, 放射線学)
• ポリアミン型薬物の腎排泄機構
• Na^+依存性担体輸送におよぼすカチオン型薬物の影響とその評価
• 理論式による多剤配合時の pH 予測方法
• リン酸ナトリウム塩の錠剤化と製剤学的評価
• ウィルソン病治療薬トリエチレンテトラミンのラットにおける消化管吸収と尿中排泄

スポンサーリンク