シベレスタット
- 関
- sivelestat sodium hydrate
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2014/10/31 09:00:53」(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 |
IV |
Identifiers |
CAS number |
127373-66-4 N |
ATC code |
None |
PubChem |
CID 107706 |
ChemSpider |
96875 Y |
UNII |
DWI62G0P59 Y |
KEGG |
D03788 Y |
ChEMBL |
CHEMBL76688 Y |
Chemical data |
Formula |
C20H22N2O7S |
Mol. 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]
Synthesis
Sivelestat is synthesised as follows:[3]
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.
- ^ K. Imaki, Y. Arai, T. Okegawa, U.S. Patent 5,017,610 (1991).
UpToDate Contents
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- 1. 急性呼吸窮迫症候群の新しい治療法 novel therapies for the acute respiratory distress syndrome
- 2. 難治性川崎病の治療 treatment of refractory kawasaki disease
English Journal
- Sivelestat relaxes vascular smooth muscle contraction in human gastric arteries.
- Amemori H, Maeda Y, Torikai A, Nakashima M.SourceDepartment of Anesthesiology and Critical Care Medicine, Saga Medical School, 5-1-1 Nabeshima, Saga, 849-8501, Japan, amemohi@cc.saga-u.ac.jp.
- Journal of physiology and biochemistry.J Physiol Biochem.2011 Dec;67(4):589-93. Epub 2011 Jul 14.
- Sivelestat sodium hydrate (sivelestat) is a novel synthetic drug and specific inhibitor of neutrophil elastase that has been approved in Japan as a treatment for acute lung injury associated with systemic inflammatory response syndrome. It is important to determine how sivelestat affects hemodynamic
- PMID 21755354
- AZD9668: pharmacological characterization of a novel oral inhibitor of neutrophil elastase.
- Stevens T, Ekholm K, Gränse M, Lindahl M, Kozma V, Jungar C, Ottosson T, Falk-Håkansson H, Churg A, Wright JL, Lal H, Sanfridson A.SourceAstraZeneca AB, Lund, Sweden.
- The Journal of pharmacology and experimental therapeutics.J Pharmacol Exp Ther.2011 Oct;339(1):313-20. Epub 2011 Jul 26.
- N-{[5-(methanesulfonyl)pyridin-2-yl]methyl}-6-methyl-5-(1-methyl-1H-pyrazol-5-yl)-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide (AZD9668) is a novel, oral inhibitor of neutrophil elastase (NE), an enzyme implicated in the signs, symptoms, and disease progression in NE-driven
- PMID 21791628
Japanese Journal
- Sivelestat併用術前化学療法によって治療しえた呼吸不全を伴うG-CSFおよびIL-6産生膀胱腫瘍の1例
- 松崎 恭介,奥見 雅由,岸本 望 [他],矢澤 浩治,宮川 康,内田 欽也,野々村 祝夫
- 泌尿器科紀要 = Acta urologica Japonica 59(7), 443-447, 2013-07
- … Neoadjuvant systemic chemotherapy was performed along with use of steroid and sivelestat, which ameliorated the respiratory distress. …
- NAID 120005308132
- A case of left pneumothorax followed by adult respiratory distress syndrome (ARDS)
- 宮原 栄治,板垣 友子,桑原 正樹,亀田 彰
- 日本呼吸器外科学会雑誌 27(1), 44-49, 2013
- … He was diagnosed with ARDS, and started treatment with corticosteroids and sivelestat sodium hydrate. …
- NAID 130003368739
- Neutrophil Elastase Inhibitor Sivelestat Attenuates Perioperative Inflammatory Response in Pediatric Heart Surgery With Cardiopulmonary Bypass:A Prospective Randomized Study
- Inoue Nobuyuki,Oka Norihiko,Kitamura Tadashi,Shibata Ko,Itatani Keiichi,Tomoyasu Takahiro,Miyaji Kagami
- International Heart Journal 54(3), 149-153, 2013
- … Sivelestat has been used clinically to treat acute lung injury associated with systemic inflammatory response syndrome. … This prospective, doubleblind, randomized study was designed to evaluate the effects of sivelestat in the perioperative period of elective pediatric open-heart surgery with CPB. … Twenty-six consecutive pediatric patients weighing between 5 and 10 kg and undergoing open-heart surgery with CPB were divided into a sivelestat group (<I>n</I> …
- NAID 130003364460
Related Links
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- シベレスタットナトリウム水和物(Sivelestat sodium hydrate) の人工心肺後炎症反応および肺障害に対する効果 Effects of neutrophil elastase inhibitor (Sivelestat sodium hydrate) on Systemic Inflammatory Response and Acute Lung ...
Related Pictures
★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
[★]
- 関
- sivelestat