Amiloride hydrochloride (盐酸阿米洛利) 是表皮钠离子通道阻断剂。
Amiloride • HCl is an inhibitor of Sodium/Potassium-ATPase Protein. It is a selective T-type calcium channel protein inhibitor that has been shown to inhibit the Polycystin-L channel, a member of the transient receptor potential (TRP) superfamily of cation channels, including the NHE. Research shows that amiloride reduces electrical potential across tubular epithelium, inhibits angiogenesis and inhibits capillary morphogenesis completely and reversibly at approximately 130 μM.
2% DMSO+caster oil
动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 | |
例如,已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法:将88 mg/kg 乘以小鼠的Km系数(3),再除以大鼠的Km系数(6),得到该药物用于大鼠的等效剂量44 mg/kg。
[1] Teiwes J, et al. Am J Hypertens, 2007, 20(1), 109-117.
[2] Jankun, J., et al. 1999. Cancer Biochem. Biophys. 17: 109-123.
[3] Loffing, J., et al. 2003. Am. J. Physiol. Renal Physiol. 284 F628-F643.
[4] Dai, X.Q., et al. 2007. Mol. Pharmacol. 72: 1576-1585.
[5] Sato, Y., et al. 2010. Anal Chim Acta. 675: 49-52.
[6] Cao, B.Y., et al. 2010. J Ethnopharmacol. 13: 122-129.
分子式 C6H9Cl2N7O |
分子量 266.09 |
CAS号 2016-88-8 |
储存方式 ﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂(常温) |
DMSO 25 mg/mL |
Water 10 mM with gentle warming |
Ethanol <1 mg/mL |
体内溶解度
NCT Number | Conditions | Interventions | Sponsor/Collaborators | Phases | Start Date | Last Updated |
NCT01802489 | Optic Neuritis|Multiple Sclerosis | Drug: Amiloride|Drug: Placebo | University of Oxford|Multiple Sclerosis Society of Great Britain and Northern Ireland | Phase 2 | 2013-02-01 | 2015-02-03 |
NCT02122731 | Hypertension|Type 2 Diabetes Mellitus|Microalbuminuria | Drug: Amiloride | Ib Abildgaard Jacobsen|Odense University Hospital | Phase 4 | 2010-11-01 | 2014-04-23 |
NCT00709137 | Hypertension | Drug: spironolactone|Drug: amiloride | VA Salt Lake City Health Care System | 2008-10-01 | 2014-05-27 | |
NCT03031496 | Hypertension | Drug: GSK3542503 (HCTZ 50mg/Amiloride HCl 5mg tablets)|Drug: Moduretic (HCTZ 50mg/Amiloride HCl 5mg tablets) | GlaxoSmithKline | Phase 1 | 2017-03-01 | 2017-03-14 |
NCT02522650 | Proteinuria | Drug: Amiloride|Drug: Triamterene | Georgetown University | Phase 4 | 2013-07-01 | 2016-11-18 |
NCT01308983 | Prehypertension | Drug: Amiloride | Augusta University | Phase 4 | 2010-09-01 | 2012-10-22 |
NCT01879527 | Optic; Neuritis, With Demyelination | Drug: Amiloride hydrochlorothiazide|Drug: Sugar pill | Medical University of Vienna | Phase 2 | 2014-03-01 | 2015-05-08 |
NCT01733680 | ADHD | Drug: amiloride|Behavioral: Behavioral | State University of New York - Upstate Medical University | Early Phase 1 | 2012-09-01 | 2014-11-19 |
NCT00274391 | Cystic Fibrosis | Drug: 7% NaCl|Drug: Amiloride HCl | University of North Carolina|Cystic Fibrosis Foundation Therapeutics|University of North Carolina, Chapel Hill | Phase 2 | 2001-07-01 | 2006-01-09 |
NCT01231165 | Coronary Heart Disease | Drug: Amiloride|Drug: Nitrates, clopidogrel, aspirin, statins | University of Carabobo|Clinical Research Unit at the Docent Institute of Urology|Northern Metropolitan Hospital|Venezuelan Foundation of Heart Failure | Phase 2|Phase 3 | 2009-02-01 | 2012-06-08 |
NCT00285805 | Insulin Resistance | Drug: Rosiglitazone versus placebo|Drug: response (sodium excretion) to amiloride infusion|Drug: response (sodium excretion) to furosemide infusion | Radboud University | 2006-02-01 | 2010-08-23 | |
NCT01388088 | Hypertension | Drug: Spironolactone|Drug: Amiloride|Drug: Placebo | Erling Bjerregaard Pedersen|Regional Hospital Holstebro | Phase 4 | 2010-09-01 | 2012-03-27 |
NCT01195805 | Essential Hypertension | Drug: Spironolactone|Other: Placebo|Drug: Amiloride | Regional Hospital Holstebro | 2010-08-01 | 2015-08-19 | |
NCT00394394 | Hypertension | Drug: Amiloride 2,5/d or Enalapril/d 10 mg | Hospital de Clinicas de Porto Alegre | Phase 2 | 2005-02-01 | 2006-10-30 |
NCT01804777 | Proteinuria|Hypertension|Type II Diabetes | Drug: Amiloride|Drug: HCTZ | University of New Mexico|Dialysis Clinic, Inc.|University of Pittsburgh | Early Phase 1 | 2013-03-01 | 2014-09-26 |
NCT01095133 | Gastroesophageal Reflux Disease|Heartburn | Drug: Amiloride|Drug: Placebo | University of North Carolina, Chapel Hill | Phase 1 | 2010-03-01 | 2012-09-18 |
NCT01918488 | Diabetic Nephropathies|Hypertension | Dietary Supplement: Standardized salt diet|Drug: Amiloride | University of Southern Denmark|Odense University Hospital|Region of Southern Denmark|The Ministry of Science, Technology and Innovation, Denmark|Danish Heart Foundation | 2013-10-01 | 2013-10-14 | |
NCT00857909 | High Blood Pressure | Drug: Amiloride|Drug: Spironolactone|Drug: Placebo|Drug: Placebo and spironolactone|Drug: Spironolactone | Regional Hospital Holstebro | Phase 1 | 2009-01-01 | 2011-07-07 |
注:以上所有数据均来自公开文献,并不保证对所有实验均有效,数据仅供参考。
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