Selectivity for Opioid Receptor Subtypes of Enkephalin Analogues in Isolated Smooth Muscle and in the Analgesic Effect in Mice
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概要
- 論文の詳細を見る
Selectivity for opioid receptor subtypes of enkephalin analogues (KK-1,-2,-3 and -4) of Tyr moiety on the N-terminal, and Phe-ol group on the C-terminal, connected with the methylene group (n=1-4) were examined in isolated smooth muscle preparations and in the analgesic effect in mice. In the longitudinal muscle preparations of guinea pig ileum (GPI), morphine, U-50488H and all the enkephalin analogues inhibited electrically evoked contractions, and the inhibitory effects of morphine, KK-1,KK-2 and KK-3 were antagonized by naloxone with relatively high pA_2 values, while that of U-50488H and KK-3 were preferentially antagonized by norbinaltorphimine. In the rabbit vas deferens preparations (RVD), on the other hand, U-50488H, KK-3 and KK-4 showed weak inhibitory effects and the inhibition of U-50488H and KK-3 were antagonized by norbinaltorphimine. By intrace-rebroventricularly (i.c.v.) injection, enkephalin analogues produced analgesia in the acetic acid (AcOH) writhing test, and the effect of KK-1 and KK-2 as well as morphine was antagonized by 1 mg/kg naloxone, while those of U-50488H and KK-3 were sensitive to 1 mg/kg Mr2266. In conclusion, enkephalin analogues with a short methylene chain between the functional groups, KK-1 and KK-2,mainly exert their effect through opioid μ-receptors, while those of longer chain, KK-3 and KK-4,act through k-receptors preferentially, and KK-3 is situated in the alternating point of the selectivity for μ-and k-receptors.
- 公益社団法人日本薬学会の論文
著者
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前田 光子
Life Science Center Faculty Of Pharmaceutical Sciences Kobe Gakuin University
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Maeda M
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Nagasaki University:faculty Of Pharmac
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KANETO Hiroshi
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Nagasaki University
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Kawasaki Koichi
Department Of Neurosurgery Kariwagun General Hospital
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KANETO Hiroshi
Emeritus Professor, Nagasaki University
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Kawasaki Keiko
Biological Science Laboratories Kao Corporation
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WATANABE Joe
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Nagasaki University
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Takahashi M
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Nagasaki University
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Takahashi Masakatsu
Department Of Pharmacoinformatics 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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MAEDA Mitsuko
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Nagasaki University
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Kawasaki Koichi
Department Of Anesthesiology And Critical Care Medicine Kagoshima University School Of Medicine
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Watanabe J
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Nagasaki University:faculty Of Pharmac
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Maeda Masatomo
Laboratory Of Biochemistry And Molecular Biology Graduate School Of Pharmaceutical Sciences Osaka Un
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Takahashi Masakatsu
Department of Analytical Research for Pharmacoinformatics, Graduate School of Pharmaceutical Sciences, Nagasaki University
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