Metadoxine
(Synonyms: 美他多辛) 目录号 : GC33771
Metadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. Metadoxine is a novel 5-HT2B receptor antagonist with a possible therapeutic role in treating ADHD.
Cas No.:74536-44-0
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
Metadoxine (Metadoxil, Metasin, pyridoxine-pyrrolidone carboxylat), also known as pyridoxine-pyrrolidone carboxylate, is a drug used to treat chronic and acute alcohol intoxication. Metadoxine is a novel 5-HT2B receptor antagonist with a possible therapeutic role in treating ADHD.
| Cas No. | 74536-44-0 | SDF | |
| 别名 | 美他多辛 | ||
| Canonical SMILES | O=C(O)[C@H](CC1)NC1=O.OCC2=C(CO)C(O)=C(C)N=C2 | ||
| 分子式 | C13H18N2O6 | 分子量 | 298.29 |
| 溶解度 | Water : ≥ 155 mg/mL (519.63 mM) | 储存条件 | Store at -20°C, stored under nitrogen |
| 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 | 3.3524 mL | 16.7622 mL | 33.5244 mL |
| 5 mM | 0.6705 mL | 3.3524 mL | 6.7049 mL |
| 10 mM | 0.3352 mL | 1.6762 mL | 3.3524 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。
Metadoxine in the treatment of acute and chronic alcoholism: a review
Int J Immunopathol Pharmacol 2003 Sep-Dec;16(3):207-14.PMID:14611722DOI:10.1177/039463200301600304.
Alcohol abuse and alcoholism are responsible for a wide variety of medical problems. The pharmaco-therapeutic aspect of alcoholism includes the use of drugs, with different actions and objectives. Among them, Metadoxine seems to be of interest. Metadoxine is able to accelerate the elimination of alcohol from the blood and tissues, to help restore the functional structure of the liver and to relieve neuro-psychological disorders associated with alcohol intoxication. Metadoxine also seems to be safe; in more than 15 years of post-marketing surveillance only minor aspecific and reversible events were monitored in patients exposed to the treatment. In this review the preclinical and clinical results obtained using Metadoxine in acute and chronic alcohol intoxication are reported.
Alternative pharmacological strategies for adult ADHD treatment: a systematic review
Expert Rev Neurother 2016;16(2):131-44.PMID:26693882DOI:10.1586/14737175.2016.1135735.
Adult Attention Deficit Hyperactivity Disorder (ADHD) is a prevalent psychiatric condition associated with high disability and frequent comorbidity. Current standard pharmacotherapy (methylphenidate and atomoxetine) improves ADHD symptoms in the short-term, but poor data were published about long-term treatment. In addition a number of patients present partial or no response to methylphenidate and atomoxetine. Research into the main database sources has been conducted to obtain an overview of alternative pharmacological approaches in adult ADHD patients. Among alternative compounds, amphetamines (mixed amphetamine salts and lisdexamfetamine) have the most robust evidence of efficacy, but they may be associated with serious side effects (e.g. psychotic symptoms or hypertension). Antidepressants, particularly those acting as noradrenaline or dopamine enhancers, have evidence of efficacy, but they should be avoided in patients with comorbid bipolar disorder. Finally Metadoxine and lithium may be particularly suitable in case of comorbid alcohol misuse or bipolar disorder.
Acute alcohol intoxication
Eur J Intern Med 2008 Dec;19(8):561-7.PMID:19046719DOI:10.1016/j.ejim.2007.06.033.
Acute alcohol intoxication is a clinically harmful condition that usually follows the ingestion of a large amount of alcohol. Clinical manifestations are heterogeneous and involve different organs and apparatuses, with behavioral, cardiac, gastrointestinal, pulmonary, neurological, and metabolic effects. The management of an intoxicated patient occurs mainly in the emergency department and is aimed at stabilizing the clinical condition of the patient, depending on his/her clinical presentation. One specific drug that is useful in the treatment of acute alcohol intoxication is Metadoxine, which is able to accelerate ethanol excretion. In patients presenting an acute alcohol intoxication, alcohol-related disorders should be detected so that the patient can be directed to an alcohol treatment unit, where a personalized, specific treatment can be established.
Hepatoprotective Effect of Metadoxine on Acetaminophen-induced Liver Toxicity in Mice
Adv Biomed Res 2018 Apr 24;7:67.PMID:29862216DOI:10.4103/abr.abr_142_17.
Background: Metadoxine (pyridoxine pyrrolidone carboxylate) is considered to be a beneficial agent for the treatment of experimental hepatotoxicity due to alcohol, CCl4, and bile duct ligation. Hence, the therapeutic effect of Metadoxine and N-acetylcysteine (NAC) as reference drug was investigated in mice exposed to acute hepatotoxicity induced by a single oral toxic dose of acetaminophen (650 mg/kg). Materials and methods: Metadoxine (200 and 400 mg/kg) and NAC (300 mg/kg) were given orally (p. o.), 2 h after acetaminophen administration. Serum aminotransferases, aspartate transaminase (AST), alanine transaminase (ALT), alkaline phosphatase (ALP), total bilirubin, hepatic glutathione (GSH), and malondialdehyde (MDA) levels were determined for evaluating the extent of hepatotoxicity due to acetaminophen and its protection by Metadoxine. Results: Findings indicated that Metadoxine significantly reduced the level of serum ALT, AST, and ALP but not total bilirubin which increased by acetaminophen intoxication. Administration of Metadoxine also attenuated oxidative stress by suppressing lipid peroxidation (MDA) and prevented the depletion of reduced GSH level which caused by acetaminophen toxicity. Besides, Metadoxine ameliorated histopathological hepatic tissue injury induced by acetaminophen. Conclusion: In most parameters examined, the effect of Metadoxine was comparable to NAC. Hence, Metadoxine could be considered as a beneficial therapeutic candidate to protect against acute acetaminophen hepatotoxicity.
Investigation of Related Impurities in Metadoxine by a Reversed Phase High Performance Liquid Chromatography Technique
Anal Sci 2021 Apr 10;37(4):581-584.PMID:33041305DOI:10.2116/analsci.20P271.
A new reversed-phase high-performance liquid chromatography (RP-HPLC) method has been developed for the separation and identification of impurities present in Metadoxine. Herein, we report that one of the impurities eluted from the Metadoxine sample is 4-deoxypyridoxine hydrochloride (4-DPH). In HPLC analysis, the retention time (RT) of 4-DPH was observed to be at 13.5 min in both the reference and Metadoxine samples and the relative retention time (RRT) was 1.71. The presence of 4-DPH in a Metadoxine sample was also confirmed by a chromatogram obtained by spiking the 4-DPH standard into the sample. Furthermore, the elution and mass of impurity 4-DPH in Metadoxine was proven by LC-mass spectroscopy studies. This method highlights the presence of another unknown impurity that has so far not been observed in earlier methods of Metadoxine evaluation. Hence, the developed method achieved superior resolution between Metadoxine and impurities and thereby facilitates the production of a purer Metadoxine drug.