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Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month.
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Win 47203
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10 mM * 1 mL/50 mg/100 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥500.0 |
|---|---|---|---|
| 规格： | 50 mg | 产品价格： | ￥415.0 |
| 规格： | 100 mg | 产品价格： | ￥658.0 |
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Milrinone
CAS No. : 78415-72-2
MCE 国际站：Milrinone
产品活性：Milrinone 是 PDE3 抑制剂，也是一种强心药、血管舒张药。
研究领域：Metabolic Enzyme/Protease
作用靶点：Phosphodiesterase (PDE)
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. 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.
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. 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.
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文献和实验是cAMP降解酶，抑制此酶活性将增加细胞内cAMP的含量，发挥正性肌力作用和血管舒张作用，临床应用已证明PDE-Ⅲ抑制药能增加心输出量，减轻心负荷，降低心肌氧耗量，缓解CHF症状。 最先应用的PDE- Ⅲ抑制药是氨力农（amrinone），临床有效，但长期口服后约15%患者出现血小板减少，可致死亡。另有心律失常、肝功能减退。现仅供短期静脉滴注用。其代替品米力农（milrinone）抑酶作用较前者强20倍，临床应用有效，能缓解症状、提高运动耐力，不良反应较少，未见引起血小
制药 磷酸二酯酶PDE- Ⅲ是cAMP降解酶，抑制此酶活性将增加细胞内cAMP的含量，发挥正性肌力作用和血管舒张作用，临床应用已证明PDE-Ⅲ抑制药能增加心输出量，减轻心负荷，降低心肌氧耗量，缓解CHF症状。 最先应用的PDE- Ⅲ抑制药是氨力农（amrinone），临床有效，但长期口服后约15%患者出现血小板减少，可致死亡。另有心律失常、肝功能减退。现仅供短期静脉滴注用。其代替品米力农（milrinone）抑酶作用较前者强20倍，临床应用有效
农（milrinone）；②血管扩张药（Vasodilators）；③b- 受体阻断药（b-blockers）；④血管紧张素转化酶抑制药（angiotensin converting enzyme inhibitor，ACEI）或AngⅡ受体阻断药（AngⅡ receptor blockers ）；⑤醛固酮拮抗药（Aldosterone antagonists）；⑥利尿药（Diuretics）等。其作用环节如图25-1所示。 正性肌力药 编辑本段 回目录 强心苷
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