Etamivan (Ethamivan)
(Synonyms: 益迷兴; Ethamivan; N,N-Diethylvanillamide) 目录号 : GC30919
A phenol with antioxidant and analeptic properties
Cas No.:304-84-7
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Ethamivan is a phenol that has been found in M. esculenta and has antioxidant and analeptic properties.1,2,3 It scavenges 2,2-diphenyl-1-picrylhydrazyl and ABTS radicals with EC50 values of 0.374 and 0.05 mg/ml, respectively, in cell-free assays.1 Ethamivan (0.25 mg/kg, i.v.) increases the respiratory rate of anesthetized cats, an effect that can be blocked by cervical vagotomy.2 Intravenous infusion of ethamivan (19.4-25.2 mg/kg) induces convulsions in conscious cats.3
1.Yi, B., Hu, L., Mei, W., et al.Antioxidant phenolic compounds of cassava (Manihot esculenta) from HainanMolecules16(12)10157-10167(2011) 2.Hirsh, K., and Wang, S.C.Respiratory stimulant effects of ethamivan and picrotoxinJ. Pharmacol. Exp. Ther.193(2)657-663(1975) 3.Luscombe, D.K., and Nicholls, P.J.Relationship between respiratory stimulant and convulsant activity of doxapram hydrochloride in conscious animalsPharmacol. Res. Commun.3(4)369-376(1971)
| Cas No. | 304-84-7 | SDF | |
| 别名 | 益迷兴; Ethamivan; N,N-Diethylvanillamide | ||
| Canonical SMILES | O=C(N(CC)CC)C1=CC=C(O)C(OC)=C1 | ||
| 分子式 | C12H17NO3 | 分子量 | 223.27 |
| 溶解度 | DMSO : ≥ 36 mg/mL (161.24 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 | 4.4789 mL | 22.3944 mL | 44.7888 mL |
| 5 mM | 0.8958 mL | 4.4789 mL | 8.9578 mL |
| 10 mM | 0.4479 mL | 2.2394 mL | 4.4789 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。
The use of ethamivan in the treatment of barbiturate poisoning
Ethamivan was used as a respiratory analeptic in the treatment of nine cases of severe barbiturate poisoning. Initial intravenous injections of 100 to 150 mg. of ethamivan increased the depth of respirations within a minute. Prolonged respiratory stimulation was achieved by a continuous intravenous infusion of 500 to 3000 mg. of ethamivan per litre of fluid. If hypotension occurred, an intravenous drip of noradrenaline was used; fluid overloading was avoided by adjusting the concentrations of drugs given, so that no more than a total of 125 c.c. of fluid per hour was administered. The chief side effect of overdosage of ethamivan was muscular twitching. This did not prove to be a problem and was of some value in determining the amount of drug given. The nine patients survived. It was concluded that ethamivan is a useful agent in the treatment of barbiturate poisoning.
Respiratory stimulant effects of ethamivan and picrotoxin
The respiratory stimulant effects of ethamivan and picrotoxin were studied in unanesthetized decerebrate cats. It was found that neither compound exhibited selective stimulant action on the respiratory neurons. Ethamivan evoked increases in respiratory rate but not in tidal volume, whereas picrotoxin profoundly altered both of these variables. The increases in respiratory rate evoked by ethamivan required intact vagus nerves since midcervical vagotomy abolished this effect. It is conceivable that ethamivan stimulated pulmonary chemoreflexes which then led to increased respiratory rate. Picrotoxin had no discernible effect on peripheral chemoreflexes. It altered, however, the central respiratory rhythmicity, or rate, depth and rhythm of respiration. There was a marked effect on central respiratory control which led to cycling between slow and deep, and rapid and shallow breathing. These were interspersed with periods of rapid and deep respiration.
Solvent dependency of rotational barriers in ethamivan and comparison to nikethamide
Carbon-13 nuclear magnetic resonance (NMR) techniques were employed to examine the effects of solvent environment on rotational barriers in two drugs known to cause widespread stimulation in the mammalian central nervous system: ethamivan and nikethamide. Total NMR bandshape analysis was performed for the exchanging alkyl carbon resonances of these compounds as a function of temperature in six solvent systems: D2O, CH3OD, CH3CH2OD, CDCl3, C6D6 and CF3CH2OH. The rate constants for rotation about the amide bond obtained in this way were used to calculate free energy (delta G++), enthalpy (delta H++) and entropy (delta S++) of activation parameters for this process. Our results indicate that the magnitude of rotational barriers is affected markedly by (1) the size and polarity of the solvent molecules, and (2) the nature of the aromatic ring system attached to the amide grouping. Comparative interpretation of the thermodynamic parameters in light of the structures of nikethamide and ethamivan (in the various solvent systems examined) has further clarified the manner in which hydrogen bonding interactions between solvent molecules and the carbonyl oxygen of these analogues stabilize transition state conformers.
Antioxidant phenolic compounds of cassava (Manihot esculenta) from Hainan
An activity-directed fractionation and purification process was used to isolate antioxidant components from cassava stems produced in Hainan. The ethyl acetate and n-butanol fractions showed greater DPPH˙and ABTS·+ scavenging activities than other fractions. The ethyl acetate fraction was subjected to column chromatography, to yield ten phenolic compounds: Coniferaldehyde (1), isovanillin (2), 6-deoxyjacareubin (3), scopoletin (4), syringaldehyde (5), pinoresinol (6), p-coumaric acid (7), ficusol (8), balanophonin (9) and ethamivan (10), which possess significant antioxidant activities. The relative order of DPPH· scavenging capacity for these compounds was ascorbic acid (reference) > 6 > 1 > 8 > 10 > 9 > 3 > 4 > 7 > 5 > 2, and that of ABTS·+ scavenging capacity was 5 > 7 > 1 > 10 > 4 > 6 > 8 > 2 > Trolox (reference compound) > 3 > 9. The results showed that these phenolic compounds contributed to the antioxidant activity of cassava.