Carrier-Mediated Uptake of Nicotinic Acid by Rat Intestinal Brush-Border Membrane Vesicles and Relation to Monocarboxylic Acid Transport
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概要
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The intestinal transport of [<14>^C]nicotinic acid was investigated at 27℃ by using brush-border membrane vesicles (BBMV) isolated from the rat small intestine. The osmolarity sensitive uptake by BBMV showed a remarkable overshoot phenomenon in the presence of an inward-directed H^+ gradient (pH_<in>=7.5,pH_<out>=6.0). In contrast, the imposition of a Na^+ gradient ([Na^+]_<in>=0 mM, [Na^+]_<out>=100 mM) had no stimulatory effect on the uptake of [<14>^C]nicotinic acid. The remarkable pH-dependence of the initial uptake showing an increase of the uptake rate with decreasing the extravesicular pH disappeared completely in the presence of a structural analogue, isonicotinic acid, at pH below 6.5. In the presence of a H^+ gradient, the initial uptake of [^<14>C] nicotinic acid was saturable with the apparent K_t of 4.43 mM and J_<max> of 2.55 nmol/mg protein/15 s. The uptake was increased by the imposition of an inside-positive membrane potential and was significantly inhibited by monocarboxylic acids such as benzoic acid, salicylic acid, acetic acid, propionic acid, valproic acid and L-lactic acids as well as two isomers (isonicotinic acid and picolinic acid). The uptake was not inhibited by nicotinamide, nicotinyl alcohol, D-glucose, p-aminohippuric acid, glycyl-L-proline, succinic acid and an exchange transport inhibitor. From these results it was concluded that nicotinic acid is transported through the intestinal brush-borde membrane by a carrier-mediated system and the system can recognize some acidic drugs with a monocarboxylic group. The pH dependent intestinal uptake of nicotinic acid can be ascribed to the proton-coupled and active carrier-mediated transport mechanism rather than a simple diffusion of the undissociated nicotinic acid to follow a pH-partition hypothesis.
- 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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Tamai I
Tokyo Univ. Sci. Tokyo Jpn
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Tamai Ikumi
Meiji Seika Kaisha Ltd. Pharmaceutical Research Center:department Of Surgery Kawasaki City Ida Hospi
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Tamai Ikumi
Faculty Of Pharmaceutical Sciences Tokyo University Of Science
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Tamai Ikumi
Department Of Pharmaceutics Faculty Of Pharmaceutical Sciences Kanazawa University
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Tamai Ikumi
Faculty Of Pharmaceutical Sciences And Hospital Pharmacy 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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SIMANJUNTAK Matheus
Faculty of Pharmaceutical Sciences, Kanazawa University
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Terasaki Tetsuya
Faculty Of Pharmaceutical Sciences Kanazawa University
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Simanjuntak Matheus
Faculty Of Pharmaceutical Sciences Kanazawa University
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