書誌事項
- タイトル別名
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- Discovery of the First in Class Drug for Intractable Itch, Nalfurafine Hydrochloride
- シンキ メカニズム ニ モトズク ナンチセイソウ ヨウショウ チリョウヤク ナルフラフィン エンサンエン ノ ソウシュツ
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抄録
Nalfurafine hydrochloride (1) was launched on March of 2009 in Japan as the first in class non-narcotic opioid drug for intractable itch caused by haemodialysis. Rational medicinal chemistry effort led us to obtain the morphinan derivative, which is a new chemical class of opioid κ-agonist without the [N-C-C-N(sp2)] pharmacophore sequence of the typical U-50488H derivatives. The applicability of “Message-Address Concept” and “Accessory Site Hypothesis” in the development of the opioid κ-agonist could also be proven. Nalfurafine hydrochloride (1) showed significant opioid κ-agonist activity and induced neither aversion nor preference in rats on the CPP (Conditioned Place Preference) test. No dependence sign was observed in monkey on the self-administration test. This compound was approved without legal narcotic nor psychotropic drug control after a clinical evaluation on human. Details on design rationale and medicinal chemistry of this novel drug will be discussed.
収録刊行物
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- 有機合成化学協会誌
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有機合成化学協会誌 68 (12), 1261-1271, 2010
公益社団法人 有機合成化学協会
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詳細情報 詳細情報について
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- CRID
- 1390001205312272384
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- NII論文ID
- 10027409446
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- NII書誌ID
- AN0024521X
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- COI
- 1:CAS:528:DC%2BC3cXhsFOgtbjL
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- ISSN
- 18836526
- 00379980
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- NDL書誌ID
- 10932714
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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
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- CiNii Articles
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- 抄録ライセンスフラグ
- 使用不可