Antinociceptive Effect and Enzymatic Degradation of Endomorphin-1 in Newborn Rat Spinal Cord.
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- Sugimoto-Watanabe Azusa
- Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd.
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- Kubota Kazufumi
- Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd.
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- Fujibayashi Kenji
- Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd.
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- Saito Koji
- Neuroscience and Immunology Research Laboratories, Sankyo Co., Ltd.
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抄録
Recently discovered endomorphin-1 and -2 are the first endogenous agonists selective for the μ-opioid receptor. We examined the antinociceptive effect and enzymatic degradation of endomorphin-1 in the newborn rat spinal cord. Endomorphin-1 inhibited the binding of [3H][D-Ala2, N-Me-Phe4, Gly-ol5] enkephalin (DAMGO) to the membrane fraction of the newborn rat spinal cord as potently as DAMGO and morphine. Endomorphin-1 at 1 - 1, 000 nM reduced the slow ventral root potential, which reflects noxious transmission in the isolated newborn rat spinal cord, concentration-dependently via the μ-opioid receptor. A similar effect was observed with endomorphin-2. The newborn rat spinal cord homogenate degraded endomorphin-1 in a 120-min incubation procedure, while it degraded [Leu5]enkephalin even in a 30-min incubation procedure. The degradation of endomorphin-1 was inhibited by actinonin but not by thiorphan. These results showed that in the newborn rat spinal cord, endomorphins had high affinity for the μ-opioid receptor and exerted μ-opioid-receptor - mediated inhibitory effects on noxious responses. Endomorphin-1 was degraded by peptidases, but slowly compared with [Leu5]enkephalin degradation, and the degrading enzymes were actinonin-sensitive peptidases.
収録刊行物
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- Jpn.J.Pharmacol.
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Jpn.J.Pharmacol. 81 (3), 264-270, 1999
公益社団法人 日本薬理学会
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詳細情報 詳細情報について
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- CRID
- 1390001204285647872
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- NII論文ID
- 10008197179
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- NII書誌ID
- AA00691188
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- COI
- 1:CAS:528:DyaK1MXns1GntLg%3D
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- ISSN
- 13473506
- 00215198
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- NDL書誌ID
- 4918250
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- PubMed
- 10622214
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可