The Opioid Receptor Selectivity for Trimebutine in Isolated Tissues Experiments and Receptor Binding Studies
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概要
- 論文の詳細を見る
Differences of affinity ot and selectivity for trimebutine between peripheral and central opioid receptors have been investigated. Trimebutine inhibited electrically induced contraction of guinea-pig ileum (GPI) and mouse vas deferens (MVD) but not of rabbit vas deferens, and the inhibition was antagonized by naloxone and, to lesser extent, by nor-binaltorphimine (nor-BNI). The pA_2 values for morphine and trimebutine with naloxone were higher than the values for these compounds with nor-BNI in both GPI and MVD preparations. GPI preparations incubated with a high concentration of morphine or trimebutine developed tolerance ; however, there was no cross-tolerance between them, suggesting difference in the underlying mechanisms. In mouse and guinea-pig brain homogenate trimebutine was about 1/13 as potent as morphine to displace the [^3H]naloxone binding, while it has no appreciable affinity for κ-opioid receptors in [^3H]U-69593,a selective κ-receptor agonist. These results suggest that trimebutine, showing its low affinity to opioid receptors, possesses μ-receptor selective properties rather than those of κ-opioid receptor in the peripheral tissues and in the central brain homogenate.
- 公益社団法人日本薬学会の論文
著者
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KANETO Hiroshi
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Nagasaki University
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KANETO Hiroshi
Emeritus Professor, Nagasaki University
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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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Watanabe J
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Nagasaki University:faculty Of Pharmac
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Takahashi Masakatsu
Department of Analytical Research for Pharmacoinformatics, Graduate School of Pharmaceutical Sciences, Nagasaki University
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