更新于：2024-04-17
Atosiban acetate
醋酸阿托西班
更新于：2024-04-17
概要
基本信息
药物类型 合成多肽 |
别名 Antocile、Antocin、Antocin II + [18] |
作用机制 AVPR拮抗剂(血管加压素受体家族拮抗剂)、OXTR拮抗剂(催产素受体拮抗剂) |
治疗领域 |
非在研适应症 |
最高研发阶段批准上市 |
首次获批日期 欧盟 (2000-01-20), |
最高研发阶段(中国)批准上市 |
特殊审评- |
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结构
分子式C43H67N11O12S2.C2H4O2 |
InChIKeySVDWBHHCPXTODI-QIWYXCRTSA-N |
CAS号914453-95-5 |
序列信息
Sequence Code 15073107
关联
34
项与 醋酸阿托西班 相关的临床试验Atosiban as a potential treatment for endometriosis - ENDOBAN pilot-study
The Effect of Selective Oxytocin Receptor Inhibitors on Endometriosis-related Pain
Effect of Oxytocin Antagonists on Implantation Success Rates of Frozen-thawed Embryo Transfer
100 项与 醋酸阿托西班 相关的临床结果
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100 项与 醋酸阿托西班 相关的转化医学
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100 项与 醋酸阿托西班 相关的专利（医药）
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479
项与 醋酸阿托西班 相关的文献（医药）2023-12-31Journal of Obstetrics and Gynaecology
Impact of prolonged use of adjuvant tocolytics after cervical cerclage on late abortion and premature delivery
Article
作者: Lu, Shu-Jing ; Xiao, Li ; Yu, Ying-Chun ; Zhao, Li-Rong ; Liu, Qing
We evaluated the impact of cervical cerclage combined with one or more uterine contraction inhibitors in persistent inhibition of uterine contraction for the treatment of late abortion and premature delivery. This retrospective case series study analysed the medical data of 58 patients who underwent cervical cerclage for cervical insufficiency and simultaneously received one or more uterine contraction inhibitors (indomethacin, ritodrine, and atosiban) and magnesium sulphate at the Zibo Maternal and Child Health Hospital between January 2019 and December 2020.Patients are normal pregnancy who received cervical cerclage without complications. The rate of successful treatment was 74.14% (43/58). The prolonged gestation duration was 16.42 ± 7.84 weeks, and the average delivery gestational age was 35.91 ± 5.16 weeks. The longest duration of treatment with a uterine contraction inhibitor or inhibitors in combination or with magnesium sulphate alone was 15.34 ± 13.16 days, and nine cases developed adverse reactions. Persistent uterine contraction inhibition after cervical cerclage could prolong pregnancy and improve pregnancy outcomes.Impact statementWhat is already known on this subject? A crucial reason for treatment failure of cervical cerclage is that uterine contraction was not effectively inhibited.What do the results of this study add? Persistent inhibition of uterine contraction after cervical cerclage prolonged pregnancy duration, increased gestational age at delivery, and improved pregnancy outcomes.What are the implications of these findings for clinical practice and/or further research? This study may provide a clinical basis for prolonging gestational age, preventing late abortion and premature delivery, and improving the survival rate and quality of life of premature infants.
2023-12-01International Journal of Biological Macromolecules
Atosiban and Rutin exhibit anti-mycobacterial activity - An integrated computational and biophysical insight toward drug repurposing strategy against Mycobacterium tuberculosis targeting its essential enzyme HemD
Article
作者: Muthu, Shivani A ; Agarwal, Meetu ; Grover, Sonam ; Sharma, Rahul ; Pahuja, Isha ; Dwivedi, Ved Prakash ; Grover, Abhinav ; Ahmad, Basir ; Mehto, Naveen Kumar
With the advancements of high throughput computational screening procedures, drug repurposing became the privileged framework for drug discovery. The structure-based drug discovery is the widely used method of drug repurposing, consisting of computational screening of compounds and testing them in-vitro. This current method of repurposing leaves room for mechanistic insights into how these screened hits interact with and influence their targets. We addressed this gap in the current study by integrating highly sensitive biophysical methods into existing computational repurposing methods. We also corroborated our computational and biophysical findings on H37Rv for the anti-mycobacterial action of selected drugs in-vitro and ex-vivo conditions. Atosiban and Rutin were screened as highly interacting hits against HemD through multi-stage docking and were cross-validated in biophysical studies. The affinity of these drugs (K ~ 106 M-1) was quantified using fluorescence quenching studies. Differential Scanning Fluorimetry (DSF) and urea-based chemical denaturation studies revealed a destabilizing effect of these drugs on target which was further validated using MD simulations. Conformational rearrangements of secondary structures were established using CD spectra and intrinsic fluorescence. Furthermore, Atosiban and Rutin inhibited M.tb growth in-vitro and ex-vivo while remaining non-toxic to mice peritoneal macrophages.
2023-11-01Biochemical Pharmacology
Non-canonical Ca2+- Akt signaling pathway mediates the antiproteolytic effects induced by oxytocin receptor stimulation in skeletal muscle
Article
作者: Cruz-Filho, João da ; Santos, José Ronaldo Dos ; Costa, Daniely Messias ; Navegantes, Luiz Carlos ; Anjos-Santos, Hevely Catharine Dos ; Santos, Tatiane de Oliveira ; Mecawi, André de Souza ; Reis, Luís Carlos ; Kettelhut, Ísis do Carmo ; Camargo, Enilton Aparecido ; Silva, Raquel Prado da ; Lauton-Santos, Sandra ; Lustrino, Danilo ; Badauê-Passos, Daniel
Although it has been previously demonstrated that oxytocin (OXT) receptor stimulation can control skeletal muscle mass in vivo, the intracellular mechanisms that mediate this effect are still poorly understood. Thus, rat oxidative skeletal muscles were isolated and incubated with OXT or WAY-267,464, a non-peptide selective OXT receptor (OXTR) agonist, in the presence or absence of atosiban (ATB), an OXTR antagonist, and overall proteolysis was evaluated. The results indicated that both OXT and WAY-267,464 suppressed muscle proteolysis, and this effect was blocked by the addition of ATB. Furthermore, the WAY-induced anti-catabolic action on protein metabolism did not involve the coupling between OXTR and Gαi since it was insensitive to pertussis toxin (PTX). The decrease in overall proteolysis induced by WAY was probably due to the inhibition of the autophagic/lysosomal system, as estimated by the decrease in LC3 (an autophagic/lysosomal marker), and was accompanied by an increase in the content of Ca2+-dependent protein kinase (PKC)-phosphorylated substrates, pSer473-Akt, and pSer256-FoxO1. Most of these effects were blocked by the inhibition of inositol triphosphate receptors (IP3R), which mediate Ca2+ release from the sarcoplasmic reticulum to the cytoplasm, and triciribine, an Akt inhibitor. Taken together, these findings indicate that the stimulation of OXTR directly induces skeletal muscle protein-sparing effects through a Gαq/IP3R/Ca2+-dependent pathway and crosstalk with Akt/FoxO1 signaling, which consequently decreases the expression of genes related to atrophy, such as LC3, as well as muscle proteolysis.
100 项与 醋酸阿托西班 相关的药物交易
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研发状态
| 适应症 | 最高研发状态 | 国家/地区 | 公司 |
|---|---|---|---|
| 早产 | 批准上市 | 冰岛 更多 | |
| 早产 | 批准上市 | 中国 更多 | |
| 1型阵发性家族性心室颤动 | 无进展 | 捷克 更多 |
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临床结果
临床结果
适应症
分期
评价
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临床1期 | - | 194 | 積餘網簾壓構製餘鑰願(衊觸鹹範壓蓋範範窪鏇) = 鏇鬱願醖鏇膚糧糧壓願 範鹽積鏇觸觸壓艱憲廠 (鏇範顧鑰齋糧願顧壓簾 ) | - | 2022-08-19 | ||
Placebo | 積餘網簾壓構製餘鑰願(衊觸鹹範壓蓋範範窪鏇) = 壓鬱簾夢鑰憲廠艱網蓋 範鹽積鏇觸觸壓艱憲廠 (鏇範顧鑰齋糧願顧壓簾 ) | ||||||
N/A | 56 | 齋糧遞繭糧齋襯淵襯艱(鑰憲選淵憲糧廠鹹襯淵) = 範鑰餘廠顧齋壓壓構選 淵製憲築糧鑰鹽網築簾 (選蓋鏇積構蓋網顧淵製 ) 更多 | - | 2018-01-01 | |||
临床1期 | - | 構鏇壓鹽願壓壓憲醖簾(齋築範選鬱壓膚餘觸繭) = 膚壓遞鏇構憲膚選衊憲 網醖窪顧繭鹹築觸淵蓋 (壓積獵構顧廠餘鏇範醖 ) 更多 | - | 2016-08-01 | |||
(Control group) | 構鏇壓鹽願壓壓憲醖簾(齋築範選鬱壓膚餘觸繭) = 構繭衊廠憲構艱鑰窪網 網醖窪顧繭鹹築觸淵蓋 (壓積獵構顧廠餘鏇範醖 ) 更多 | ||||||
N/A | 800 | 夢製願齋襯糧餘蓋獵壓(顧構糧鏇壓觸鏇願憲齋) = 淵顧餘窪醖築鏇夢膚餘 襯夢積膚鹽淵廠襯網繭 (鹹築壓製餘鏇鹽獵製餘 ) | - | 2014-12-01 | |||
Placebo | 夢製願齋襯糧餘蓋獵壓(顧構糧鏇壓觸鏇願憲齋) = 壓積廠構範糧衊夢製膚 襯夢積膚鹽淵廠襯網繭 (鹹築壓製餘鏇鹽獵製餘 ) | ||||||
临床1期 | - | 71 | 膚齋選顧願築膚壓願築(壓鹹獵鏇衊選衊鹹積壓) = 壓鬱願鬱糧膚積鹹糧鹽 衊衊觸鹹餘觸積衊選壓 (構選繭廠願鹽鏇鹽顧餘 ) 更多 | - | 2012-09-01 |
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