产品说明书
Rilmenidine phosphate
 |
同义名 : | - |
| CAS号 : | 85409-38-7 | |
| 货号 : | A866594 | |
| 分子式 : | C10H19N2O5P | |
| 纯度 : | 98%+ | |
| 分子量 : | 278.24 | |
| MDL号 : | MFCD00875846 | |
| 存储条件： |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 4 mg/mL(14.38 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO H2O: 85 mg/mL(305.49 mM)，配合低频超声助溶 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | α2-Adrenoceptors (α2-AR) found in the cardiomyocyte's sarcolemma represent a very important negative feedback for control of myocardial contractility by endogenous catecholamines[2]. Rilmenidine is a clinically approved anti-hypertensive agent that acts by activating ADRA2/α2-adrenoceptors and imidazoline-1 receptors (I1Rs) in the brain and periphery. It can be a mTOR-independent autophagy inducers. Stable inducible PC12 cells expressing either wild-type (23Q) or expanded polyglutamine (74Q) huntingtin both showed a significant increase in LC3-II (microtubule-associated protein 1 light chain) when treated with rilmenidine for 24 h[3]. Sinus rate, corrected sinus recovery time (CSRT) and Wenckebach point (WP) were measured in seven intact dogs. Atrial rate and atrial effective refractory period (AERP) were measured in six atrioventricular (AV)-blocked dogs with ventricular pacing. Each dog received with at least a three-day interval rilmenidine as dihydrogen phosphate in four successive intravenous injections, 30 min apart. In intact dogs, rilmenidine was administered at 50, 50, 100 and 200 μg/kg. In AV-blocked dogs, doses of rilmenidine were 25, 25, 50 and 100 μg/kg. Rilmenidine decreased sinus rate and atrial rate from the first dose. A lengthening of CSRT and a lowering of WP were observed at all doses with rilmenidine. A shortening of AERP was also seen with rilmenidine from the second dose[4]. | ||
| 临床研究 | |||||
|---|---|---|---|---|---|
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT02539810 | Hypertension ... 展开 >>Hypertension Resistant to Conventional Therapy Angiographically Proven Grade III Unilateral or Bilateral Atherosclerotic Renal Artery Stenosis (ARAS) Greater Than or Equal to 60 Percent 收起 << | Phase 4 | Terminated | - | France ... 展开 >> Hopital Pasteur Nice, Alpes-Maritimes, France, 06002 Hopital Saint Andre - CHU Bordeaux Bordeaux, Gironde, France, 33075 Hopital Rangueil - CHU Toulouse Toulouse, Haute-Garonne, France, 31059 Hopital Lapeyronie - CHU Montpellier Montpellier, Herault, France, 34295 Hopital Arthur Gardiner Dinard, Ille-et-Vilaine, France, 35800 Hopital Pontchaillou - CHU Rennes Rennes, Ille-et-Vilaine, France, 35033 Groupe Hospitalier Mutualiste Grenoble, Isere, France, 38028 Hopital Michallon - CHU Grenoble La Tronche, Isere, France, 38700 Institut Lorrain du Cœur et des Vaisseaux Louis Mathieu Vandoeuvre les Nancy, Meurthe-et-Moselle, France, 54500 Hopital de Brabois Vandoeuvre les Nancy, Meurthe-et-Moselle, France, 54511 Hopital Cardiologique - CHRU Lille Lille, Nord, France, 59037 CHU Clermont-Ferrand Clermont-Ferrand, Puy-de-Dome, France, 63000 Hopital de la Croix-Rousse - CHU Lyon Lyon, Rhone, France, 69004 Hopital de la Pitie Salpetriere Paris, France, 75013 Hopital Europeen Georges Pompidou (HEGP) Paris, France, 75015 收起 << |
| NCT00892892 | Chronic Kidney Disease ... 展开 >> Hypertension 收起 << | Phase 4 | Withdrawn | - | Germany ... 展开 >> University of Erlangen-Nuremberg, CRC, med. Clinic 4 Erlangen, Bavaria, Germany, 91054 收起 << |
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
3.59mL 0.72mL 0.36mL |
17.97mL 3.59mL 1.80mL |
35.94mL 7.19mL 3.59mL |
| 参考文献 |
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