Mefexamide
(Synonyms: 美非沙胺) 目录号 : GC31003
Mefexamide是一种特别的精神刺激剂。
Cas No.:1227-61-8
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
Mefexamide is a particular psychostimulant.
| Cas No. | 1227-61-8 | SDF | |
| 别名 | 美非沙胺 | ||
| Canonical SMILES | O=C(NCCN(CC)CC)COC1=CC=C(OC)C=C1 | ||
| 分子式 | C15H24N2O3 | 分子量 | 280.36 |
| 溶解度 | Soluble in DMSO | 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 | 3.5668 mL | 17.8342 mL | 35.6684 mL |
| 5 mM | 0.7134 mL | 3.5668 mL | 7.1337 mL |
| 10 mM | 0.3567 mL | 1.7834 mL | 3.5668 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。
[Contribution to biotransformation and analysis of the psychopharmacon mefexamide (author's transl)]
Z Rechtsmed.1981;87(1-2):117-27.PMID:7303940DOI: 10.1007/BF00201216.
After oral administration of a therapeutic dosage (400 mg) Mefexamide (I), six excretion products were detected in human urine and subsequently identified by GC/MS and TLC: in addition to the unchanged drug (I) in the acidic extracted urine without hydrolysis p-methoxiphenoxiaceticacid-methylester (II) and p-methoxiphenoxiaceticacid (III) were detected; the latter two and p-hydroxyanisole (IV) were also found in the acidic extract after hydrolysis (with hydrochloric acid or enzymatic). In the alkaline urine extract besides the unchanged drug (I) and the main metabolite V (partially described previously by Forist et al. [8]1), metabolite VI, which occurred only in very small amounts, could be detected. Additionally, 2-diethylaminoethylamine (VII) was identified as an artifact in the alkaline extract after acidic hydrolysis. Hydrolysis of mefexamide with hydrochloric acid led to substances II, III, IV, and VII. For the main metabolite V, a synthesis route is described. Approximately 15% of the administered drug was recovered in the 24-h urine; substances I and V could be detected a least 72h after application.
[Quantitative determination of mefexamide and its main degradation product desmethyl-mefexamide in human urine after ingestion of therapeutic doses (author's transl)]
Z Rechtsmed.1981;87(4):297-303.PMID:7340287DOI: 10.1007/BF00200645.
After oral ingestion of 400 mg Mefexamidehydrochloride for Mefexamide (I) and its main degradation product Desmethyl-Mefexamide (II) the following pharmakokinetic parameters have been determined: 1. Elimination of I and II follows 1st order kinetics. 2. Biological half-life t 1/2 for I is 4-6, for II 4.5-6.5 H. 3. Elimination rate constant for I and II is between 0.10 to 0.20 h-1. 4. 5-10% of the administered drug are excreted unchanged, 10-16% as Desmethyl-Mefexamide within 72 h after ingestion. 5. The described thinlayer chromatographic and gas chromatographic/mass spectrometric methods allow detection of I and II for at least 72 h after application. 6. II is excreted free and conjugated in nearly equal amounts.
[Experimental study on the tracking behaviour with a view to differentiating the effects of an antidepressant in various doses compared to placebo (author's transl)]
Arzneimittelforschung.1976;26(12):2235-42.PMID:1037281
In a double-blind cross-over study 15 highly motivated, healthy male subjects (Ss), aged from 23 to 29 years, were given 200 mg and 400 mg p-methoxy-phenoxyaceticacid-diethylaminoethylamide-hydrochloride (mefexamide) and a placebo. On each of the three days the Ss were tested in different tracking devices and the integrated absolute error was measured in the tests of a duration of three hours each. Influences of practice, leading to unwanted and disturbing effects were excluded by a preceding period of four training sessions on different days. The main result of the investigation was that performance in tracking was ambivalent. The single dosage (200 mg mefexamide) caused small improvements in tracking in the range of about 5%. These differences from placebo partly could be determined to be significant at the level of 5% compared to placebo. The double dosage (400 mg mefexamide) deteriorated tracking performance significantly (5%-and partly 1%-level, two-tailed test) in the range of about 10% on the average. Differences in performance between the two dosages were correspondingly larger and could be determined at a higher level of significance, too.
[Further study and the comparative characteristics of potential stimulants of higher nervous activity]
Farmakol Toksikol.1982 Sep-Oct;45(5):108-11.PMID:7140947
The most active stimulants of the higher nervous activity (nootropil, tonibral, mefexamide, sydnocarb, pyrroxane, ethimizole, gutimin and analogs) were studied and compared as regards their effects on the time course of forming the conditioned reflex of avoidance in rats during one-time and "fraction" learning. The models of special retraining were used to examine the drug effects on the phases of consolidation and the time course of the reflex reproduction. The most active compounds have been defined in terms of the parameters under consideration.
[Use of the conditioned avoidance reflex for detecting potential stimulants of higher nervous activity and their comparative characteristics]
Farmakol Toksikol.1982 Jul-Aug;45(4):5-9.PMID:7128785
Comparative research has been made of the influence of psychostimulants (amphetamine, sydnocarb, centedrin), neurotropic agents (neutrophil, mefexamide, tonibral, acephen), analeptics (ethimizole), alpha-adrenoblockers (pyrroxane), glutamine and its analogues on the forming in rats of the avoidance conditioned reflex in a Y-shaped labyrinth and its reproduction (repeated learning) after 24 hours. The time of learning, the number of mistakes and runnings until the criterion of learning is attained, emotional status, motor activity, elements of individual and group behavior of the animals have been studied to reveal the drugs having the most pronounced effect on the characteristics examined.