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The opioid activity and receptor selectivity of fluorinated Leu5 Enkephalin analogues in vitro and in vivo.
http://hdl.handle.net/10069/38850
http://hdl.handle.net/10069/3885024de096f-03ce-4d5a-858f-7342883da4bb
名前 / ファイル | ライセンス | アクション |
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JPD14_101.pdf (601.1 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 | The opioid activity and receptor selectivity of fluorinated Leu5 Enkephalin analogues in vitro and in vivo. | |||||
言語 | ||||||
言語 | eng | |||||
キーワード | ||||||
主題Scheme | Other | |||||
主題 | naltrindole | |||||
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× TOKUYAMA, Shogo× TAKAHASHI, Masakatsu× KANETO, Hiroshi× MAEDA, Mitsuko× KAWASAKI, Koichi× TAGUCHI, Takeo× KOBAYASHI, Yoshiro× YAMAMOTO, Yoshihiro× SHIMOKAWA, Kazuhiro |
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抄録 | ||||||
内容記述タイプ | Abstract | |||||
内容記述 | The opioid activity and the selectivity for opioid receptor (subtypes) of newly synthesized fluorinated enkephalin (Enk) analogues, [2R, 4R], [2R, 4S], [2S, 4S] and [2S, 4R] trifluoro-Leu5-Enk (KKF-31, 32, 33 and 34) were investigated. The inhibitory effect of KKF-compounds on the electrically induced contractions of guinea-pig ileum (GPI) and mouse vas deferens (MVD) were dosedependent but relatively lower than that of L-Leu5-Enk, except that KKF-34 was rather slightly more potent than L-Leu5-Enk in MVD preparations. In GPI preparations, the pA2 values of naloxone for these compounds were higher than those of naltrindole while the values of naltrindole for KKF-compound were higher than those of naloxone in MVD preparations. Intracerebroventricular KKF-31 and KKF-32 at doses of 20 and 10 nmol/mouse, respectively, produced analgesia comparable to 0.1 nmol Tyr-D-Arg-Phe-Lys-NH2 and 100 nmol Tyr-D-Thr-Gly-Phe-Leu-Thr; however, neither KKF-33 nor 34 produced analgesia up to the doses of 100 nmol/mouse. Both naloxone, 1 mg/kg, i.p., and naltrindole, 10 mg/kg, i.p., antagonized KKF-31- and KKF-32-induced analgesia. The results suggest that the introduction of trifluoromethyl group in Leu5 results in the alternation of the opioid activity and receptor selectivity. Although KKF-33 and KKF-34 possessed a more potent in vitro inhibitory effect than KKF-31 and KKF-32, mediated through μ- and δ-opioid receptors in both preparations, they did not show any appreciable analgesic effect. KKF-31 and KKF-32 produce naloxone-and naltrindole-reversible analgesia irrespective of in vitro μ- and δ-opioid activity. | |||||
書誌情報 |
Journal of Pharmacobio-Dynamics 巻 14, 号 2, p. 101-105, 発行日 1991 |
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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/bpb1978.14.101 | |||||
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, 14(2), pp.101-105; 1991 |