書誌事項
- タイトル別名
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- Pharmacological profile of sendide, a tachykinin NK-1 receptor antagonist.
- ニューロキニン 1 ジュヨウタイ キッコウヤク センダイド ノ ヤクリガクテキ
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説明
Progress in the characterization of tachykinin receptors and the understanding of the physiological and pathological roles of tachykinins is highly dependent on the discovery of potent and selective antagonists with metabolic stability. We have recently described a peptidic antagonist of the tachykinin NK 1 receptor, sendide (Tyr-D-Phe-Phe-D-His-Leu-Met-NH2), that is a selective and extremely potent antagonist of NK-1 receptors, but displays no antagonistic activity on the response induced by NK-2 or NK-3-receptor agonists in the mouse spinal cord. When coadministered with substance P (SP) intrathecally (i.t.), sendide markedly inhibited the scratching, biting and licking behavior induced by SP in a dose-dependent manner. The antagonistic effect of sendide on the SP-induced behavioral response was approximately 7300 times more potent than that of CP-96, 345, a non-peptidic NK-1-receptor antagonist. The duration of the antagonistic effect of sendide was longer than that of CP-96, 345. The behavioral response elicited by other NK-1-receptor agonists, septide, physalaemin and [Sar9, Met (O2)11]-SP, was reduced significantly by a small dose of sendide. In the [3H]-SP binding assay using mouse spinal cord membranes, sendide potently displaced [3H]-SP binding, with a potency approximately 5.4×104 times greater than that of CP-96, 345. Moreover, Lt. administration of sendide was found to produce the antinociceptive effect through the blockage of NK-1 receptors in the mouse formalin and capsaicin tests. Sendide is therefore likely to become a powerful pharmacological tool for studying the functional roles of NK-1 receptors in the central nervous system.
収録刊行物
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- 日本薬理学雑誌
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日本薬理学雑誌 110 (6), 315-324, 1997
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
- 1390001204272679936
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- NII論文ID
- 10005708977
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- NII書誌ID
- AN00198335
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- COI
- 1:CAS:528:DyaK2sXnslarsb0%3D
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- ISSN
- 13478397
- 00155691
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- NDL書誌ID
- 4355520
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- PubMed
- 9503389
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- 本文言語コード
- ja
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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