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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2015/06/26 00:00:32」(JST)
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Sivelestat
|
Systematic (IUPAC) name |
N-{2-[({4-[(2,2-dimethylpropanoyl)oxy]phenyl}sulfonyl)amino]benzoyl}glycine |
Clinical data |
AHFS/Drugs.com |
International Drug Names |
Legal status
|
|
Routes of
administration
|
IV |
Identifiers |
CAS Registry Number
|
127373-66-4 N |
ATC code
|
None |
PubChem |
CID: 107706 |
IUPHAR/BPS |
6441 |
ChemSpider |
96875 Y |
UNII |
DWI62G0P59 Y |
KEGG |
D03788 Y |
ChEMBL |
CHEMBL76688 Y |
Chemical data |
Formula |
C20H22N2O7S |
Molecular mass
|
434.46 g/mol |
SMILES
- CC(C)(C)C(=O)OC1=CC=C(C=C1)S(=O)(=O)NC2=CC=CC=C2C(=O)NCC(=O)O
|
InChI
-
InChI=1S/C20H22N2O7S/c1-20(2,3)19(26)29-13-8-10-14(11-9-13)30(27,28)22-16-7-5-4-6-15(16)18(25)21-12-17(23)24/h4-11,22H,12H2,1-3H3,(H,21,25)(H,23,24) Y
Key:BTGNGJJLZOIYID-UHFFFAOYSA-N Y
|
N (what is this?) (verify) |
Sivelestat (INN, research name ONO 5046, marketed as Elaspol) is an inhibitor of human neutrophil elastase.[1]
It is used in the treatment of acute respiratory failure[2] and preliminary studies show it may also improve neuropathic pain.[3]
Synthesis
Sivelestat is synthesised as follows:[4]
References
- ^ Kawabata K, Suzuki M, Sugitani M, Imaki K, Toda M, Miyamoto T (June 1991). "ONO-5046, a novel inhibitor of human neutrophil elastase". Biochem. Biophys. Res. Commun. 177 (2): 814–20. doi:10.1016/0006-291X(91)91862-7. PMID 2049103.
- ^ Imokawa S; Mori K; Harada M et al. (June 2008). "[Acute respiratory failure due to pneumocystis pneumonia successfully treated with combined use of sivelestat sodium hydrate]". Nihon Kokyuki Gakkai Zasshi (in Japanese) 46 (6): 461–5. PMID 18592991.
- ^ Weyer, Andy D.; Stucky, Cheryl L. (May 2015). "Repurposing a leukocyte elastase inhibitor for neuropathic pain". Nature Medicine 21 (5): 429–430. doi:10.1038/nm.3861. ISSN 1078-8956.
- ^ K. Imaki, Y. Arai, T. Okegawa, U.S. Patent 5,017,610 (1991).
English Journal
- The effect of the neutrophil elastase inhibitor sivelestat on early injury after liver resection.
- Tsujii S, Okabayashi T, Shiga M, Takezaki Y, Sugimoto T, Kobayashi M, Hanazaki K.SourceDepartment of Surgery, Kochi Medical School, Kohasu-Okocho, Nankoku, Kochi, 783-8505, Japan.
- World journal of surgery.World J Surg.2012 May;36(5):1122-7. doi: 10.1007/s00268-012-1501-8.
- BACKGROUND: The effects of sivelestat on endotoxin-induced lung injury, postperfusion lung injury, and ischemia-reperfusion are known, yet the benefits of sivelestat during liver surgery have yet to be elucidated. The aim of the present study was to assess the effects of sivelestat, with a focus on
- PMID 22366983
- Prognostic impact of clinical course-specific mRNA expression profiles in the serum of perioperative patients with esophageal cancer in the ICU: a case control study.
- Takahashi S, Miura N, Harada T, Wang Z, Wang X, Tsubokura H, Oshima Y, Hasegawa J, Inagaki Y, Shiota G.SourceDivision of Anesthesiology and Critical Care Medicine, Tottori University School of Medicine, Nishicho 36-1, Yonago, Tottori 683-8503, Japan.
- Journal of translational medicine.J Transl Med.2010 Oct 22;8:103. doi: 10.1186/1479-5876-8-103.
- BACKGROUND: We previously reported that measuring circulating serum mRNAs using quantitative one-step real-time RT-PCR was clinically useful for detecting malignancies and determining prognosis. The aim of our study was to find crucial serum mRNA biomarkers in esophageal cancer that would provide pr
- PMID 20969744
- [Case of fulminant idiopathic interstitial pneumonia treated by sodium siverlestat (Elaspol) and steroid pulse therapy following extracorporeal lung assist (ECLA)].
- Morooka T, Morioka M, Nomura Y, Furuya H.SourceMedical Center for Emergency and Critical Care, Nara Prefectural Nara Hospital Nara 631-0846
- Masui. The Japanese journal of anesthesiology.Masui.2007 Oct;56(10):1193-7.
- A patient with fulminant idiopathic interstitial pneumonia was treated by sodium siverlestat and steroid pulse therapy following extracorporeal lung assist (ECLA). On arriving at the emergency room, Pa(O2) was 44.5 mmHg under oxygen with 10 l reserver mask, and emergency intubation was performed. X-
- PMID 17966626
Japanese Journal
- PS-100-4 ブタ肝切除モデル用いた虚血再灌流障害,肝再生に対するElaspolの効果(PS-100 ポスターセッション(100)肝臓:基礎-1,第111回日本外科学会定期学術集会)
- 喜島 博章,下田 貢,岩崎 喜実,岡田 としえ,澤田 登起彦,窪田 敬一
- 日本外科学会雑誌 112(臨時増刊号_1・2), 678, 2011-05-25
- NAID 110008685006
- Sivelestat Sodium Hydrate (Elaspol) の妊娠子宮頸管熟化抑制作用
- 杉山 将樹,大槻 克文,松浦 玲,新城 梓,八鍬 恭子,中山 健,満川 香織,千葉 博,長塚 正晃,岡井 崇
- 日本周産期・新生児医学会雑誌 = Journal of Japan Society of Perinatal and Neonatal Medicine 45(1), 67-71, 2009-04-25
- NAID 10025167578
- Sivelestat Sodium Hydrateとエンドトキシン吸着療法との併用療法が有用であったARDSの1例
- 兼田 裕司,矢田 清吾,山口 剛史 [他]
- 四国医学雑誌 63(1/2), 54-57, 2007-04-25
- … We report here a case of Acute Respiratory Distress Syndrome(ARDS)due to perforation ofthe sigmoid colon, for which therapy with Sivelestat Sodium Hydrate(SSH, Elaspol)and PolymyxinB-immobilized Direct Hemoperfusion(PMX-DHP)was shown to be effective. …
- NAID 110006283065
Related Links
- 1 ─. 〔組成・性状〕. 〔効能・効果〕. 全身性炎症反応症候群に伴う急性肺障害の改善. 〈 効能・効果に関連する使用上の注意〉. 1 .本剤は下記の(1)および(2)の両基準を 満たす患者に投. 与すること。 (1)全身性炎症反応症候群に関しては、以下の項目の うち、.
- Ono Pharmaceutical Co., Ltd. (Headquarters: Osaka City, President: Kimiichiro Matsumoto) will launch Elaspol® 100 for injection, the world's first drug for acute lung injury associated with systemic inflammatory response syndrome (SIRS), ...
Related Pictures
![Systematic ( IUPAC ) name](https://1mg.info/0/6/d/2497.jpg)
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![Elaspol® for Injection for the Treatment](https://1mg.info/0/6/d/2501.jpg)
★リンクテーブル★
[★]
- 英
- sivelestat
- 化
- シベレスタットナトリウム水和物 sivelestat sodium hydrate
- 関
- エラスポール Elaspol
効能又は効果
- 注射用エラスポール100
作用機序
- 注射用エラスポール100
- 好中球エラスターゼは蛋白分解酵素の一つであり、肺に集積した好中球から遊離される。好中球エラスターゼは肺結合組織を分解し、肺血管透過性を亢進させ、急性肺障害を誘発させる。また、好中球遊走因子の産生を促進し、炎症反応を増幅させ、全身性炎症反応症候群に伴う急性肺障害における重要な障害因子として注目されている。本剤は、好中球エラスターゼの選択的な阻害剤である。
参考
- http://www.info.pmda.go.jp/go/pack/3999422D1020_1_08/3999422D1020_1_08?view=body