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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 pA2 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. 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Selectivity for opioid receptor subtypes of enkephalin analogues in isolated smooth muscle and in the analgesic effect in mice.
http://hdl.handle.net/10069/38848
http://hdl.handle.net/10069/3884827b33d6c-f08a-449f-a8b8-1706920418f5
名前 / ファイル | ライセンス | アクション |
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JPD12_544.pdf (563.3 kB)
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Item type | 学術雑誌論文 / Journal Article(1) | |||||
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公開日 | 2019-02-21 | |||||
タイトル | ||||||
タイトル | Selectivity for opioid receptor subtypes of enkephalin analogues in isolated smooth muscle and in the analgesic effect in mice. | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | analgesic effect | |||||
資源タイプ | ||||||
資源タイプ識別子 | http://purl.org/coar/resource_type/c_6501 | |||||
資源タイプ | journal article | |||||
著者 |
WATANABE, Joe
× WATANABE, Joe× TAKAHASHI, Masakatsu× MAEDA, Mitsuko× KAWASAKI, Koichi× KANETO, Hiroshi |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | 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 pA2 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. | |||||
書誌情報 |
Journal of Pharmacobio-Dynamics 巻 12, 号 9, p. 544-548, 発行日 1989 |
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出版者 | ||||||
出版者 | 日本薬学会 | |||||
出版者別言語 | ||||||
Pharmaceutical Society of Japan | ||||||
ISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 0386846X | |||||
EISSN | ||||||
収録物識別子タイプ | ISSN | |||||
収録物識別子 | 18811353 | |||||
書誌レコードID | ||||||
収録物識別子タイプ | NCID | |||||
収録物識別子 | AA00704585 | |||||
DOI | ||||||
関連タイプ | isIdenticalTo | |||||
識別子タイプ | DOI | |||||
関連識別子 | 10.1248/bpb1978.12.544 | |||||
権利 | ||||||
権利情報 | c The Pharmaceutical Society of Japan | |||||
著者版フラグ | ||||||
出版タイプ | VoR | |||||
出版タイプResource | http://purl.org/coar/version/c_970fb48d4fbd8a85 | |||||
引用 | ||||||
内容記述タイプ | Other | |||||
内容記述 | Journal of Pharmacobio-Dynamics, 12(9), pp.544-548; 1989 |