Etimizol
(Synonyms: Ethimizole; Ethymisol; Ethymisole) 目录号 : GC36013
Etimizol(Ethymisole; Antiffine; Ethylnorantifein) 可有效地作用于缺氧造成的失忆症。
Cas No.:64-99-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Etimizol(Ethymisole; Antiffine; Ethylnorantifein) was shown to relieve amnesia effectively in the origin of which there is the hypoxic component (hypobaric hypoxia, actinomycin D, mechanical injury of the brain).
The time interval between administration ofetimizol (3 mg/kg) and the onset of learning varied between 0.5 and 3 h in the several series. Etimizol (Ethymisole) did not facilitate the learning in rats whatever the time of administration and biological modality of reinforcement [1]. After administration of Etimizol (Ethymisole) at doses of 10 or 1 mg/loop mean residence time of etimizol in the loop was 20.1 and 7.6 min, respectively, with mean standard deviation being 3.1 and 0.8, respectively [2]. Extracellular application of 5--10 mM/L Etimizol (Ethymisole) exerted a specific effect on the giant neurons of the Coretus corneus isolated nervous system: action potential duration increased significantly, speed of development of its descending phase decreased, as well as the trace hyperpolarization amplitude [3].
[1]. Borisova GIu. Effect of etimizol on instrumental learning in rats. Biull Eksp Biol Med. 1985 Jun;99(6):705-6. [2]. Trnovec T, et al. Etimizol absorption from the small intestine in dogs: the dependence on dosage. Biull Eksp Biol Med. 1986 Dec;102(12):729-30. [3]. Vislobokov AI, et al. Elektrophysiological parameters of mollusk neurons under the influence of etimizol. Fiziol Zh SSSR Im I M Sechenova. 1975 Jun;61(6):917-24.
| Cas No. | 64-99-3 | SDF | |
| 别名 | Ethimizole; Ethymisol; Ethymisole | ||
| Canonical SMILES | O=C(C1=C(C(NC)=O)N(CC)C=N1)NC | ||
| 分子式 | C9H14N4O2 | 分子量 | 210.23 |
| 溶解度 | Ethanol: ≥ 33.33 mg/mL (158.54 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 | 4.7567 mL | 23.7835 mL | 47.567 mL |
| 5 mM | 0.9513 mL | 4.7567 mL | 9.5134 mL |
| 10 mM | 0.4757 mL | 2.3783 mL | 4.7567 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。
[Etimizol absorption from the small intestine in dogs: the dependence on dosage]
Biull Eksp Biol Med 1986 Dec;102(12):729-30.PMID:3801627doi
As Etimizol has been previously reported to be of low bioavailability, the kinetics of its absorption from the dog intestinal loop was investigated in chronic experiments. After administration of Etimizol at doses of 10 or 1 mg/loop mean residence time of Etimizol in the loop was 20.1 and 7.6 min, respectively, with mean standard deviation being 3.1 and 0.8, respectively. It was concluded that overall Etimizol absorption from small intestine was high and its low bioavailability resulted from presystemic drug metabolism, as well as that the absorption kinetics was dose-dependent, with saturation reached at higher drug doses.
[Effect of Etimizol on instrumental learning in rats]
Biull Eksp Biol Med 1985 Jun;99(6):705-6.PMID:4016262doi
The action of Etimizol on the acquisition of the conditioned reflexes with different complexity and biological significance of reinforcement was studied. The acquisition was performed in a shuttle box and U-shaped maze using food and footshock stimuli. The time interval between administration of Etimizol (3 mg/kg) and the onset of learning varied between 0.5 and 3 h in the several series. Etimizol did not facilitate the learning in rats whatever the time of administration and biological modality of reinforcement. It is suggested that the positive effect of Etimizol on the memory is related to its influence on the consolidation stage.
[The significance of the antihypoxic properties of Etimizol in its nootropic action]
Farmakol Toksikol 1988 Sep-Oct;51(5):27-30.PMID:3145213doi
The antihypoxic effects of Etimizol and other nootropics are analysed on various experimental models of hypoxia and during bicycle ergometric exercise in healthy volunteers. Etimizol was shown to relieve amnesia effectively in the origin of which there is the hypoxic component (hypobaric hypoxia, actinomycin D, mechanical injury of the brain). The advantage of Etimizol as compared to other nootropics with similar action (meclofenoxate, piracetam) is its high effectiveness at a single administration.
[Dynamics of the distribution of labeled Etimizol in brain cell structures]
Biull Eksp Biol Med 1983 Oct;96(10):53-5.PMID:6626731doi
The time course of 14C-etimizol distribution in cell structures of the rat cerebral cortex was studied. Two minutes after intraperitoneal injection Etimizol penetrates brain cells. At this time the greater portion of the drug is found in cytosol. In five minutes the maximal part of the label gets bound with cell nuclei and microsomal protein fraction extracted with 0.14 M NaCl. These two cell fractions show the highest radioactivity throughout the entire observation period (up to 7 days). Since these fractions are reported to be capable of calcium accumulation, a suggestion is made that metabolic effects of Etimizol are likely to be related to calcium metabolism.
[Elektrophysiological parameters of mollusk neurons under the influence of Etimizol]
Fiziol Zh SSSR Im I M Sechenova 1975 Jun;61(6):917-24.PMID:1132537doi
Extracellular application of 5--10 mM/L Etimizol exerted a specific effect on the giant neurons of the Coretus corneus isolated nervous system: action potential duration increased significantly, speed of development of its descending phase decreased, as well as the trace hyperpolarization amplitude. The effect was reversible and depended upon the Etimizol concentration and the initial functional state of neurons. Etimizol is supposed to decrease the K-+ permeability of neurons' membrane during action potential. Large concentrations of Etimizol decrease, probably, the Na+ permeability as well as suggested by reducing maximum of the ascending phase of action potential.