Amrinone
(Synonyms: 氨力农; Inamrinone) 目录号 : GC42792
An inhibitor of PDE3
Cas No.:60719-84-8
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Amrinone is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 19.5 µM). It increases developed tension and contractile force in isolated cat papillary muscle. Amrinone (1-10 mg/kg) has positive inotropic effects, increasing the rate and force of heart contraction in anesthetized and unanesthetized dogs.
| Cas No. | 60719-84-8 | SDF | |
| 别名 | 氨力农; Inamrinone | ||
| Canonical SMILES | NC1=CC(C2=CC=NC=C2)=CNC1=O | ||
| 分子式 | C10H9N3O | 分子量 | 187.2 |
| 溶解度 | DMF: 0.3 mg/ml,DMSO: 0.5 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 5.3419 mL | 26.7094 mL | 53.4188 mL |
| 5 mM | 1.0684 mL | 5.3419 mL | 10.6838 mL |
| 10 mM | 0.5342 mL | 2.6709 mL | 5.3419 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Amrinone: is it the inotrope of choice?
J Cardiothorac Anesth 1989 Dec;3(6 Suppl 2):45-57.PMID:2521051DOI:10.1016/0888-6296(89)90059-8.
In the treatment of acute heart failure, conventional therapy with epinephrine, norepinephrine, dopamine, and dobutamine may be used effectively to treat inotropic abnormalities. However, the addition of a vasodilator to catecholamine therapy may be needed to help improve lusitropic function. Because it seems to exert positive inotropic and lusitropic effects, the phosphodiesterase inhibitor Amrinone may be a valuable addition to the anesthesiologist's armamentarium for the treatment of acute heart failure. When used as adjunctive therapy with catecholamines, Amrinone has been shown to exert a significant additive and synergistic effect. Amrinone may also be the inotrope of choice in patients who are refractory to therapy with conventional inotropes, due to its positive inotropic and lusitropic effects, combined with its vasodilating effects. Because of its broad pharmacodynamic spectrum, Amrinone may effectively control all of the major elements involved in myocardial performance--preload, afterload, contractility, and heart rate.
Amrinone: pharmacokinetics and pharmacodynamics
J Cardiothorac Anesth 1989 Dec;3(6 Suppl 2):10-4.PMID:2521045DOI:10.1016/0888-6296(89)90054-9.
Amrinone is a selective inhibitor of phosphodiesterase fraction 3 in both cardiac and smooth muscle. Intravenous administration in humans produces increased contractility and vasodilation of venous capacitance and arterial conductance vessels. The elimination half-life in healthy patients is reported to be 2.6 to 4.1 hours, making it the only long-acting positive inotropic agent available that can be administered either as an intravenous bolus or by infusion. A low incidence of side effects, often minor, has been reported with intravenous use. Thrombocytopenia does not seem to be a problem with short-term use. Amrinone represents a new approach in the pharmacologic therapy for ventricular dysfunction following cardiac surgery.
Amrinone metabolism
Clin Pharmacol Ther 1981 Mar;29(3):394-401.PMID:7471610DOI:10.1038/clpt.1981.54.
High-performance liquid chromatographic methods for the analysis of Amrinone in plasma and for both Amrinone and its N-acetyl metabolite in urine were developed and applied to measure specimens obtained from a number of healthy men who had received intravenous or oral Amrinone. The intravenous doses ranged from 0.8 to 2.2 mg/kg. Terminal elimination of Amrinone from the bloodstream followed apparent first-order kinetics. Half-life, after the drug had distributed to the tissues, was estimated by a log-linear least-squares regression; mean half-life was 2.6 +/- 1.4 hr. During the first 24 hr after medication, unchanged Amrinone excreted in the urine of these subjects represented 10% to 40% of the dose. N-Acetyl metabolite in the urine represented less than 2% of the dose. In the oral study, doses ranged from 25 to 250 mg (0.31 to 3.5 mg/kg) and the maximum plasma concentration attained was proportional to the dose. The first order terminal elimination half-life was possibly dose-related. In only one subject were there unequivocal amounts of the N-acetyl metabolite in the plasma.
The role of Amrinone in potential heart transplant patients with pulmonary hypertension
J Cardiothorac Anesth 1989 Dec;3(6 Suppl 2):33-7.PMID:2521049DOI:10.1016/0888-6296(89)90057-4.
Orthotopic heart transplantation is contraindicated in patients with pulmonary hypertension and an elevated pulmonary vascular resistance. In an attempt to make otherwise unacceptable patients possible candidates for heart transplantation, Amrinone was administered intravenously to 27 individuals with a transpulmonary gradient and pulmonary vascular resistance in the abnormal range. Twenty-four of 27 patients (89%) responded positively. Twenty-one of 27 (78%) went on to transplantation and 20 of 21 (95%) survived the procedure. A second study compared Amrinone therapy with conventional therapy in 38 potential transplant candidates with pulmonary hypertension. Amrinone was more effective in reducing pulmonary hypertension than conventional therapy with high-dose diuretics, digitalis, and captopril (86% v 63%). Survival rate of those awaiting transplantation was also significantly higher in the Amrinone group (91% v 63%). Although the protocol for comparing the two regimens does not allow for extrapolation of the results (Amrinone was administered in-hospital under close monitoring, whereas conventional therapy was self-administered at home), the findings confirm the clinical impression that Amrinone seems more effective and safer than conventional therapy in the treatment of potential heart transplant patients with pulmonary hypertension.
Perioperative experience with Amrinone
Eur J Anaesthesiol Suppl 1992;5:15-9.PMID:1600963doi
Amrinone is the only phosphodiesterase fraction III inhibitor currently available in the USA for the treatment of perioperative biventricular failure. Patients with chronic congestive heart failure (CHF) show down-regulation of the beta 1-adrenergic receptor with a decrease in receptor density and altered responses to catecholamines. Intravenous administration of Amrinone can transiently restore beta 1-adrenergic responses in patients who have CHF. Amrinone's mechanism of vasodilatation, independent of the beta 1-adrenergic receptor, nitrates, and calcium entry blockers, proves an important therapeutic option for pulmonary hypertension. The elimination half-life of Amrinone in volunteers is 2.6-4.1 h, and 3.5 h when administered into the cardiopulmonary bypass (CPB) circuit. Different loading and infusion doses have been reported for Amrinone. Investigators have demonstrated that increases in cardiac output following Amrinone administration are directly related to plasma concentration. In cardiac surgical patients, following a dose of 0.75 mg kg-1 administered into the CPB circuit, plasma concentrations are subtherapeutic after 10 min. We believe that, when using Amrinone to facilitate separation from CPB, a bolus dose of 1.5 mg kg-1 or more should be administered. If therapeutic levels need to be maintained in patients with biventricular failure, an infusion should also be administered after the bolus dose. Additive effects have been demonstrated when catecholamines are administered concomitantly with Amrinone and other PDE III inhibitors to increase cyclic AMP in cardiac muscle and improve contractility. The use of Amrinone with catecholamines is also important clinically, because together they attenuate the vasoconstrictive effects of catecholamines alone, while the catecholamines support perfusion pressure. Amrinone represents a novel drug for managing biventricular dysfunction in cardiac surgical patients.