Heptaminol hydrochloride (RP-2831 hydrochloride)
(Synonyms: 6-氨基-2-甲基-2-庚醇盐酸盐,RP-2831 hydrochloride) 目录号 : GC32515
An aliphatic amine with cardiotonic and sympathomimetic activities
Cas No.:543-15-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Heptaminol is an aliphatic amine with cardiotonic and sympathomimetic activities.1,2,3 It decreases the amplitude of peak calcium currents by 30% in isolated guinea pig ventricular myocytes when used at a concentration of 100 ?M.1 Heptaminol inhibits norepinephrine uptake and induces catecholamine release in primary bovine chromaffin cells.3,2 It increases blood pressure in cats when administered intravenously at a dose of 15 mg, an effect that can be blocked by reserpine .4
1.Peineau, N., Mongo, K.G., Le Guennec, J.-Y., et al.Alteration of the L-type calcium current in guinea-pig single ventricular myocytes by heptaminol hydrochlorideBr. J. Pharmacol.107(1)104-108(1992) 2.Grobecker, H.On the mode of action of heptaminolNaunyn Schmiedebergs Arch Pharmakol.266(4)339-340(1970) 3.Delicado, E.G., Fideu, M.D., Miras-Portugal, M.T., et al.Effect of tuamine, heptaminol and two analogues on uptake and release of catecholamines in cultured chromaffin cellsBiochem. Pharmacol.40(4)821-825(1990) 4.Garrett, J., Osswald, W., and Goncalves Moriera, M.Mechanism of cardiovascular actions of heptanolaminesBr. J. Pharmacol. Chemother.18(1)49-60(1962)
| Cas No. | 543-15-7 | SDF | |
| 别名 | 6-氨基-2-甲基-2-庚醇盐酸盐,RP-2831 hydrochloride | ||
| Canonical SMILES | CC(O)(C)CCCC(N)C.[H]Cl | ||
| 分子式 | C8H20ClNO | 分子量 | 181.7 |
| 溶解度 | DMSO : ≥ 100 mg/mL (550.36 mM) | 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。 |
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| 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 5.5036 mL | 27.5179 mL | 55.0358 mL |
| 5 mM | 1.1007 mL | 5.5036 mL | 11.0072 mL |
| 10 mM | 0.5504 mL | 2.7518 mL | 5.5036 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 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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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。
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Use of Heptaminol hydrochloride for catecholamine weaning in septic shock
Am J Ther 2012 Jan;19(1):e8-17.PMID:20720484DOI:10.1097/MJT.0b013e3181e9b630.
We analyze in the current study the impact of Heptaminol hydrochloride (Heptamyl) administration in patients with septic shock requiring adrenergic support on the duration of vasopressor infusion and on catecholamine delay weaning. In this prospective study were included 49 nonconsecutive patients with septic shock requiring vasopressor infusion and with stable hemodynamic parameters during more than 24 hours. All these patients were included in a random way to receive or not Heptaminol hydrochloride. The primary end point was the effect of Heptaminol hydrochloride administration on duration of weaning, defined as cessation of vasopressor support. There were 32 males (65%) and 17 females (35%). The mean age (± standard deviation) was 53.9 ± 22.2 years. Norepinephrine was the most commonly used vasopressor agent (73.4%). The comparison between two groups (with and without Heptaminol hydrochloride) showed that two groups had the same epidemiologic, clinical, and biologic findings on intensive care unit admission. In our study, we found that the introduction of Heptamyl was associated with a quick decrease of dose of dopamine and norepinephrine in comparison with the Heptamyl-free group. By comparing the two groups, we found that the delay of catecholamine weaning was significantly faster for the dopamine (P = 0.008) and noradrenalin (P = 0.001) in the Heptamyl group. Finally, the intensive care unit mortality rate and the hospital mortality rate were significantly lower in the Heptamyl group. Our study shows a reduction in norepinephrine and dopamine weaning duration in septic patients enrolled in the Heptaminol hydrochloride group.
Action of Heptaminol hydrochloride on contractile properties in frog isolated twitch muscle fibre
Br J Pharmacol 1991 Nov;104(3):714-8.PMID:1724630DOI:10.1111/j.1476-5381.1991.tb12493.x.
1. Heptaminol stopped or delayed the progressive decline in tension which characterizes the phenomenon of fatigue in frog isolated twitch muscle fibre. 2. Heptaminol had no action on the sodium, potassium and calcium voltage-dependent ionic conductances. 3. The hypothesis of an action via an internal alkalinization was tested by comparison with the action of NH4Cl. Both substances increased the tension. 4. The action of heptaminol was suppressed in sodium-free (TRIS) solution or in the presence of amiloride while the action of NH4Cl was always observed. 5. These results could be explained by a stimulation of the Na/H antiport by heptaminol.
Decrease in internal H+ and positive inotropic effect of Heptaminol hydrochloride: a 31P n.m.r. spectroscopy study in rat isolated heart
Br J Pharmacol 1989 Dec;98(4):1233-40.PMID:2611491DOI:10.1111/j.1476-5381.1989.tb12669.x.
1. The cardiotonic effect of Heptaminol hydrochloride (Hept-a-myl, Delalande) was studied using 31P-nuclear magnetic resonance (n.m.r.) spectroscopy and left ventricular pressure (LVP) measurements in rat isolated hearts. The possibility of this effect being mediated by an intracellular realkalinisation was tested. 2. Isolated hearts were perfused at 10 ml min-1 by the Langendorff method with Krebs-Henseleit solution at 37 degrees C and stimulated at 5 Hz. Mechanical activity was measured as variations of left ventricular pressure (LVP). 31P-n.m.r. spectra were recorded every 2 min. Changes in cardiac adenosine triphosphate (ATP), phosphocreatine (PCr) and inorganic phosphate (Pi) were followed and intracellular pH (pHi) was estimated from the chemical shift of Pi. 3. The effects of heptaminol were tested in different conditions: normoxia, moderate ischaemia, severe ischaemia, and moderate ischaemia in the presence of amiloride or guanidinium chloride as inhibitors of the Na-H exchange. 4. In normoxia, heptaminol induced a cyclic increase of systolic LVP, associated with an increase in Pi. No significant effect on pHi was observed. In changing from normoxia to moderate ischaemia, PCr and systolic LVP decreased; a mild intracellular acidification (pHi 6.96) was obtained. Heptaminol induced a restoration of pHi and increased LVP. In severe ischaemia, the realkalinization effect and the restoration of LVP induced by heptaminol were no longer observed. During moderate ischaemia, Na-H exchange inhibitors decreased pHi and LVP. Heptaminol applied in the presence of these inhibitors was unable to restore pHi and LVP. In severe ischaemia, the realkalinization effect and the restoration of LVP induced by heptaminol were no longer observed. During moderate ischaemia, Na-H exchange inhibitors decreased pHi and LVP. Heptaminol applied in the presence of these inhibitors was unable to restore pHi and LVP. 5. These results suggest that the positive inotropic effect of heptaminol during moderate ischaemia could be related to a restoration of internal pH, possibly mediated by a stimulation of the Na-H exchange.
Alteration of the L-type calcium current in guinea-pig single ventricular myocytes by Heptaminol hydrochloride
Br J Pharmacol 1992 Sep;107(1):104-8.PMID:1422567DOI:10.1111/j.1476-5381.1992.tb14470.x.
1. The effects of heptaminol on calcium current amplitude and characteristics were studied in single ventricular myocytes of guinea-pig by use of the whole cell configuration of the patch clamp technique. 2. A concentration-dependent decrease in ICa amplitude was observed. At heptaminol concentration as low as 10(-6) M, this effect was observed in only two cells (n = 6). At 10(-5) M the reduction of ICa was of 30 +/- 15% (n = 11). 3. The current recovery from inactivation at -40 mV holding potential (HP) seemed less sensitive to perfusion with heptaminol (greater than 10(-6) M). However, at -80 mV HP the overshoot of the recovery curve was decreased by heptaminol. 4. Both at -40 mV and -80 mV HP, heptaminol (10(-5) M) significantly increased the steady state inactivation of ICa. 5. As previously proposed by others to explain the effects of membrane active substances, the effects of heptaminol may result from alterations in cell membrane properties and possibly from an increase in intracellular free calcium ion concentration.
Condensation of Heptaminol hydrochloride for its spectrofluorimetric determination in pure form and tablets: application in human plasma
Luminescence 2020 Sep;35(6):821-826.PMID:31994292DOI:10.1002/bio.3787.
A sensitive, simple, accurate and less expensive fluorimetric method was designed and validated for analysis of heptaminol HCl in both its pure and dosage forms, as well as in human plasma. The main principle used in the proposed approach was the condensation reaction between heptaminol's primary amino moiety and ethyl acetoacetate/formaldehyde reagents, giving a derivative that was highly fluorescent at 416 nm after excitation at 350 nm. Various experimental parameters that affected either the product's development or its stability were evaluated and optimized. The constructed calibration curve was linear over the range 0.2-2 μg/ml, with a good correlation coefficient (0.9996). Both the calculated limit of detection and limit of quantitation were 0.06 and 0.18 μg/ml, respectively. The presented approach was a success when used to determine Corasore® tablets and was validated according to International Council for Harmonisation guidelines.