Characteristic Subcellular Distribution, in Brain, Heart and Lung, of Biperiden, Trihexyphenidyl, and (-)-Quinuclidinyl Benzylate in Rats
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概要
- 論文の詳細を見る
The subcellular distribution of biperiden (BP), trihexyphenidyl (TP) and (-)-quinuclidinyl benzylate (QNB) in brain, heart and lung following high dose (3.2mg/kg) i.v. administration was investigated in rats. The subcellular distribution of BP or TP used clinically conformed with that of QNB, a typical potent central muscarinic antagonist. The concentration-time courses of the brain subcellular fractions for these drugs were of two types which decreased slowly and in parallel to the plasma concentration. The subcellular distribution in the brain and heart was dependent on the protein amount of each fraction. The percent post-nuclear fraction (P_2) of the total concentration in the lung was characteristically about 3-5 times larger than that in the heart. It was elucidated that the distribution in the lung differs from that in the brain and heart, with high affinity which is not dependent on the protein amount in the P_2 fraction containing lysosomes. On the other hand, at a low dose (650ng/kg) of ^3H-QNB, each fraction as a percentage of the total concentration in the brain increased in synaptic membrane and synaptic vesicles and decreased in nuclei and cytosol as compared with the high dose. These results show that although the tissue concentration-time courses of anticholinergic drugs appear to decrease simply in parallel to plasma concentration, the subcellular distribution exhibits a variety of patterns among various tissues.
- 公益社団法人日本薬学会の論文
- 1998-01-15
著者
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YOKOGAWA Koichi
Department of Hospital Pharmacy, School of Medicine, Kanazawa University
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Nakashima E
Dep. Of Pharmaceutics Kyoritsu Univ. Of Pharmacy
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Nakashima Emi
Faculty Of Pharmaceutical Sciences Kanazawa University
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Nakashima Emi
Department Of Pharmaceutics Kyoritsu University Of Pharmacy
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Nakashima Emi
Department Of Pediatrics:hospital Pharmacy:and Faculty Of Pharmaceutical Sciences University Of Kana
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Ichimura F
Hospital Pharmacy Kanazawa University
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Ichimura Fujio
Department Of Pediatrics:hospital Pharmacy:and Faculty Of Pharmaceutical Sciences University Of Kana
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Ishizaki Junko
Hospital Pharmacy Kanazawa University
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Ishizaki Junko
Department Of Clinical Drug Informatics Faculty Of Pharmaceutical Sciences Kanazawa University
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OHKUMA SHOJI
Department of Biochemistry, Faculty of Pharmaceutical Sciences, Kanazawa University
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Nakashima Emi
Faculty Of Pharmaceutical Sciences And Hospital Pharmacy Kanazawa University
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Yokogawa Koichi
Department Of Clinical Pharmaceutics Graduate School Of Pharmaceutical Sciences Kanazawa University
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Yokogawa Koichi
Department Of Hospital Pharmacy Kanazawa University Hospital
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Yamamoto K
Faculty Of Pharmaceutical Sciences Josai University
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Ohkuma S
Kanazawa Univ. Ishikawa Jpn
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Ohkuma Shoji
Department Of Biochemistry Faculty Of Pharmaceutical Sciences Kanazawa University
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Ichimura Fujio
Hospital Pharmacy Kanazawa University
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Yokogawa Koichi
Department Of Chemistry Faculty Of Pharmaceutical Sciences Hokuriku University
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中島 恵美
Department Of Pharmaceutics Kyoritsu University Of Pharmacy
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