生物活性 | |||
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描述 | Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Topical Enoximone (25 μg; intratracheal route) abrogates house dust mite (HDM)-induced allergic airway inflammation. The Enoximone-treated (25 μg; for 5 days) HDM-exposed mice shows significant reductions in inflammatory cell numbers including eosinophils, macrophages, neutrophils, ILC2s, and T cells, indicating that Enoximone treatment reduces airway inflammation[1]. Enoximone sulphoxide has the same inotropic and vasodilator activities as enoximone but is 0.13-0.14 times as potent and has a 13 times longer duration of inotropic action in the dog[2]. Early intervention with the selective PDE3-inhibitor enoximone may help to revert respiratory failure as well as avert mechanical ventilation, and reduces ICU/hospital time in patients with severe SARS-CoV-2 pneumonia[4]. Twelve weeks of treatment with low-dose enoximone improves exercise capacity in patients with CHF(chronic heart failure), without increasing adverse events[5]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT03772990 | Cardiac Surgery ... 展开 >> Cardiopulmonary Bypass 收起 << | Phase 4 | Not yet recruiting | March 30, 2022 | - |
NCT01864252 | Myocardial Reperfusion Injury | Phase 3 | Unknown | February 2016 | United Kingdom ... 展开 >> The Heart Hospital, UCL Hospitals NHS Trust Recruiting London, United Kingdom, NW1 2PG Contact: Ashraf Hamarneh, MBchB,MRCP 02034479781 a.hamarneh@ucl.ac.uk Principal Investigator: Derek M Yellon, PhD DSc FACC Principal Investigator: Derek J Hausenloy, MD PhD FRCP Sub-Investigator: Ashraf Hamarneh, MBchB MRCP Sub-Investigator: Shyam Kolvekar, MS MCh FRCS Sub-Investigator: Roger Cordery, BSc FRCA Sub-Investigator: Vivek Sivaraman, MRCP MD FRCA 收起 << |
NCT00484133 | Severe Sepsis ... 展开 >> Microcirculation 收起 << | Phase 4 | Unknown | - | Netherlands ... 展开 >> Onze Lieve Vrouwe Gasthuis, intensive care Recruiting Amsterdam, Netherlands, 1090 HM Contact: Rutger v Raalte, MD 0031205993007 R.vanRaalte@olvg.nl Principal Investigator: Rutger v Raalte, MD 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
4.03mL 0.81mL 0.40mL |
20.14mL 4.03mL 2.01mL |
40.27mL 8.05mL 4.03mL |
参考文献 |
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