SPECIFIC INHIBITORS FOR PROLYL ENDOPEPTIDASE AND THEIR ANTI-AMNESIC EFFECT
スポンサーリンク
概要
- 論文の詳細を見る
Several peptides and peptide derivatives were tested for their inhibitory effect on prolyl endopeptidase and possible properties as anti-amnesic agents. Among the compounds tested, Z-Gly-Pro-CH_2Cl, Z-Val-prolinal, Boc-Pro-prolinal, Z-Pro-prolinal, aniracetam and pramiracetam inhibited the enzyme activities at K_i values in the order of nM to μM, and the effect of the prolinal-containing peptide derivatives was specific for prolyl endopeptidase. Z-Pro-prolinal was the most effective inhibitor in vitro (K_i=5 nM) and in vivo (50 to 70% inhibition in various organs of rat at a dose of 1 μmol/animal i.p.). Regional differences were observed in the effect of inhibitors on the brain enzyme activities : most active in mesencephalon, followed by striatum, cerebellum, hippocampus, hypothalamus ; and inactive in cerebral cortex and medulla oblongata. In the passive avoidance learning test using rats, pretreatment with Z-Pro-prolinal prevented the induction of amnesia by scopolamine at the dose of 1 μmol/animal, i.p. Z-Val-prolinal, Z-Pyr-prolinal and Z-Gly-Pro-CH_2Cl were also effective in the retention test at 24 and 48 h after the training trial. The antiamnesic effect of these compounds was approximately parallel to the in vitro inhibitory activities on prolyl endopeptidase. These results suggest the possibility that the inhibitors exhibit their anti-amnesic effect through the regulation of the enzyme activity in the brain.
- 公益社団法人日本薬学会の論文
著者
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Tsuru Daisuke
Department of Applied Microbiology, Kumamoto Institute of Technology
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YOSHIMOTO Tadashi
Department of Animal Husbandry, Miyagi Prefectural Agricultural Experiment Station, Sendai
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Yoshimoto T
Nagasaki Univ. Nagasaki Jpn
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Yoshlmoto Tadashi
School Of Pharmaceutical Sciences Nagasaki University
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Yoshimoto Tadashi
School Of Pharmaceutical Sciences Nagasaki University
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Yoshimoto Tadashi
School Of Pharmaceutical Sciences Nagasaki University:yakult Central Institute For Microbiological R
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Yoshimoto Tadashi
School Of Pharmaceutical Sciences Nagasiki University
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KANETO Hiroshi
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Nagasaki University
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KADO KUNIO
Departments of Biotechnology and Pharmacology, School of Pharmaceutical Sciences, Nagasaki Universit
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MATSUBARA FUTOSHI
Departments of Biotechnology and Pharmacology, School of Pharmaceutical Sciences, Nagasaki Universit
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KORIYAMA NOBUHIRO
Departments of Biotechnology and Pharmacology, School of Pharmaceutical Sciences, Nagasaki Universit
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Kado K
School Of Pharmaceutical Sciences Nagasaki University:yakult Central Institute For Microbiological R
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Tsuru D
School Of Pharmaceutical Sciences Nagasaki University:yakult Central Institute For Microbiological R
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Tsuru Daisuke
Department Of Applied Microbial Technology Sojo University
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Tsuru Daisuke
Department Of Applied Microbial Technology Kumamoto Institute Of Technology
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KANETO Hiroshi
Emeritus Professor, Nagasaki University
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Koriyama Nobuhiro
Departments Of Biotechnology And Pharmacology School Of Pharmaceutical Sciences Nagasaki University:
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Kaneto H
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Nagasaki University
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Kaneto Hiroshi
Department Of Pharmacology Faculty Of Pharmaceutical Science Nagasaki University
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Yoshimoto Tomotaka
Department Of Forest Products Faculty Of Agriculture The University Of Tokyo
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Yoshimoto Tadashi
Department Of Animal Husbandry Miyagi Prefectural Agricultural Experiment Station Sendai
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Matsubara Futoshi
Departments Of Biotechnology And Pharmacology School Of Pharmaceutical Sciences Nagasaki University:
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Yoshimoto Tadashi
Department Of Advanced Bioscience Faculty Of Agriculture Kinki University
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Matsubara Futoshi
Department of Microbiology and Biochemistry, Daiichi College of Pharmaceutical Sciences
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