| CAS |
No.78415-72-2 |
| 中文名称 |
米力农(10mM in DMSO,无菌） |
| 英文名称 |
Milrinone(10mM in DMSO，Sterile） |
| 分子式 |
C12H9N3O |
| 分子量 |
211.22 |
| 溶解性 |
请根据自己的实验要求使用。 |
| 外观(性状) |
无菌溶液 |
| 储存条件 |
Stroe at -20℃，6 months. |
| 靶点 |
Phosphodiesterase (PDE) |
| 通路 |
Metabolic Enzyme&Protease |
| 背景说明 |
Milrinone 是 PDE3 抑制剂。 |
| 生物活性 |
Milrinone is a PDE3 inhibitor， and also an inotrope and vasodilator.[1-4] |
| In Vitro |
Milrinone (1 μM) increases PKA activity in hypoxic myocytes to normoxic levels. Milrinone (50 nM) normalizes TP receptor sensitivity in hypoxic myocytes by restoring PKA-mediated regulatory TP receptor phosphorylation[1]. Milrinone significantly reduces NE-induced vasoconstriction， attenuating both NE sensitivity and maximal tension generation. Inhibition of ATP-sensitive K+ channels or voltage-gated K+ channels do not prevent the milrinone-induced attenuation of NE responses[4]. |
| In Vivo |
Milrinone (1 μg/kg/min， i.v.) significantly reduces PAP， PVR (?18.96 ± 1.7%)， and LAP (?26.03 ± 2.3%) in congestive heart failure (CHF) rats. Milrinone (1 mg/mL， inhalation) results in a near-maximal reduction of PAP without significant effects on AP， decreases pulmonary artery pressure similarly in a larger collective of CHF rats. Milrinone inhalation selectively increases cAMP but not cGMP plasma concentrations in both groups. Repeated milrinone inhalations even reduce lung wet/dry weight ratio[2]. Milrinone (49.5 μg) largely shifts the ESPVR upwards and significantly increases end-systolic pressure (ESP(0.08)) and the systolic pressure-volume area (PVA(0.08)) at a mid-range LV volume (0.08 mL/g myocardium). Milrinone also slightly decreases LV ESP(ESV) and decreased Ea[3]. |
| 动物实验 |
In juvenile rats of 100 ± 8 g body weight (bw)， CHF is induced by supracoronary aortic banding. In brief， rats are anesthetized by intraperitoneal injection of ketamine (87 mg/kg bw) and xylazine (13 mg/kg bw). Rats are placed in the supine position， the chest wall is shaved， and a left thoracotomy is performed in the third intercostal space during ventilation with 100% O2. The ascending aorta is freed from connective tissue and partially occluded by implantation of a titanium clip with a defined internal diameter of 0.8 mm. After surgical closure of the thorax， the rats are allowed to recover from anesthesia. For postoperative analgesia， rats receive 250 mg/kg bw of metamizole intramuscularly immediately after the operation and on the first postoperative day. Sham-operated rats serve as controls. After recovery from anesthesia， the animals are placed in cages with free access to water and standard laboratory diet. For inhalation， milrinone (0.2-5 mg/mL) or NaCl (0.9%) are nebulized using an ultrasonic nebulizer and inhaled for 3 min at identical peak inspiratory pressures as used throughout the experiment. A 3-min nebulization of 1 mg/mL milrinone results in vaporization of 14 μg of the phosphodiesterase-3 inhibitor as determined by microgravimetry. Therefore， the respective dose of 39 μg/kg is analog to inhaled doses in human studies. For intravenous delivery， milrinone (initial bolus of 2-10 μg/kg， followed by 0.2-1 μg/kg/min) or equivalent volumes of NaCl (0.9%; initial bolus of 1.6 mL/kg， followed by 10 μL/kg/h) are administered by an infusion pump for 10 min. |
| 数据来源文献 |
[1]. Santhosh KT， et al. Milrinone attenuates thromboxane receptor-mediated hyperresponsiveness in hypoxic pulmonary arterial myocytes. Br J Pharmacol. 2011 Jul;163(6):1223-36.
[2]. Hentschel T， et al. Inhalation of the phosphodiesterase-3 inhibitor milrinone attenuates pulmonary hypertension in a rat model of congestive heart failure. Anesthesiology. 2007 Jan;106(1):124-31.
[3]. Kishi T， et al. Effects of milrinone on left ventricular end-systolic pressure-volume relationship of rat hearts in situ. Clin Exp Pharmacol Physiol. 2001 Sep;28(9):737-42.
[4]. Taylor MS， et al. Effect of milrinone on small mesenteric artery vasoconstriction: role of K(+) channels. Am J Physiol. 1999 Jul;277(1 Pt 1):G69-78. |
| 规格 |
1ml |
| 单位 |
瓶 |
中文
英语
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