Emoxypine Succinate (Mexidol), ≥98%

Emoxypine

Chemical Information: 

Technical Information:  

Background:

Emoxypine is a pyridoxine derivative used in research for its purported antioxidant effects. In Russia, it is used medically for anxiolytic, anticonvulsant, neuroprotective, cognition-enhancing, and anti-inflammatory effects. PubChem classifies this compound broadly in the groups of: platelet aggregation inhibitors, antioxidant, and psychotropic compounds.

It was first synthesized in Russia in the 1980s, at the in the Institute of Biochemical Physics. The addition of the succinate chemical group is said to be of great significance to the compound’s effects – for example, for being employed as a substrate for cellular energy. According to the Russian Emoxypine website, its most important mechanisms are its antioxidant and membranotropic effects.

Modes of action:

Emoxypine is an effective antioxidant with additional membrane-protecting effects. According to the Russian website providing information on the compound, it acts through several key mechanisms. These include:

1. Inhibiting free radical oxidation (scavenging effects)
2. Increasing the activity of endogenous antioxidant enzymes (for example, superoxide dismutase)
3. Inhibiting free radical synthesis in several biochemical systems (for example, during the synthesis of prostaglandin)
4. Regulating lipids in the body (for example, reducing the cholesterol to phospholipid ratio and shifting structure transition into low-temperature zones)
5. Modulating the activity of membrane receptors like phosphodiesterase, cyclic nucleotides, adenylate cyclase, aldoreductase, and acetylcholinesterase.
6. Increasing the binding ability of benzodiazepine, GABA, and acetylcholine receptors
7. Providing stability to membrane structures
8. Increasing dopamine and monoamine synthesis in the brain

Animal studies indicated that the compound is effective at reducing the products of lipid peroxidation, including low-density lipoproteins (LDLs) and total cholesterol. Further, studies have indicated that the compound has effective inhibitory effects on the aggregation of blood platelets (anti-clotting effects). Finally, studies have indicated a dose-dependent increase in average coronary blood flow.

Further Scientific research:

Several clinical trials have been conducted to evaluate the safety and efficacy of this compound. Below, we list a few of these studies for reference. Please note that this is by no means a comprehensive account of the available literature. For more information, please check search results for Emoxypine on PubChem.

Clinical Reviews:

A 2009 article reviewed the available literature on Emoxypine use for the treatment of brain damage resulting from stroke. Researchers found a strong correlation between the production of reactive oxygen species (free radicals) and products of lipid peroxidation and the extent of damage occurring from ischemic stroke. Furthermore, results from previous clinical studies indicate that the use of Emoxypine has preventative effects pre-stroke, and can be used to prevent further damage (through antioxidant effects) post-stroke.

Human studies: 

In 2017, a randomized, double-blind, placebo-controlled study was conducted to evaluate the safety and efficacy of Emoxypine. 151 patients with a history of ischemic stroke were enrolled and assigned to two groups: the first received 500 mg/day by IV, for 10 days, followed by 125mg, three times daily, for 8 weeks. the second group received placebo. The results showed a statistically significant difference in improvement of measured outcomes for the first group compared to the second. This included improvements in quality of life and movement. Furthermore, no significant difference in adverse effects was recorded between the groups.

In a 2016 study, the antihypoxic efficacy of Emoxypine during carotid endarterectomy (CE) procedure was examined in 54 patients with cerebral atherosclerotic stenosis. The results showed that, compared to placebo, Emoxypine significantly reduces brain hypoxia, the overall time of surgery, and the neurological and psychological status of patients, post-surgery.

A 2014 study examined the effects of Emoxypine-containing toothpaste and mouthwash on participants with xerostomia (excessively dry mouth) symptoms. Results showed that, after one year of use, the experimental group had 2.7 times lower reported oral mucosa disorders.

In a 2016 study, Russian researchers conducted a study to explore the effects of Emoxypine on 110 patients with primary hypothyroidism. Neurological and psychological outcomes were measured and electroneuromyography was performed to assess the status of the peripheral nervous system. Significant positive effects were recorded for all parameters in the experimental group.

In terms of anticonvulsant effects, a 2013 study examined 75 participants with symptomatic focal posttraumatic epilepsy. They were administered a combination of Emoxypine and phenotropil (Phenibut). The results showed a significant reduction in the number of seizures as well as improvements in quality of life and cognitive performance. This is reportedly in contrast to most nootropics, which typically aggravate seizures.

A 2013 study used a combination of 100 – 300 mg Emoxypine with 150 mg picamilon to examine the effects in patients with primary open-angle glaucoma (POAG), over a period of 14-21 days. Results showed improvements in visual acuity and increased blood flow in the central retinal artery, for the experimental groups.

The effects of antidepressant medication alone and in combination with Emoxypine was studied in 70 patients with panic disorder and insomnia. After two weeks of treatment, results showed a significant difference in anxiolytic and sleep-promoting effects between the two groups, with the combination treatment having better outcomes.

Anti-inflammatory effects were studied in a group of patients with rheumatoid arthritis. After two weeks of treatment, the experimental group showed improvements in inflammation markers, as well as quality of life and a reduction in depressive symptoms.

Animal studies:

Due to a large number of studies available on human participants, animal studies have been excluded from this summary. For more information, please search on PubMed, and select “Other Animals”.

Toxicity Cases:

No toxicity reports were found for this compound.

Precautions and Disclaimer:
This Material is Sold For Laboratory and Research Use Only.  Not for Diagnostic or Therapeutic, Drug, or Other Household Uses.

References:

¹ "Emoxypine Succinate.” (2018). Compound Summary for CID 122298. PubChem, Open Chemistry Database, US National Library of Medicine. Available online from  https://pubchem.ncbi.nlm.nih.gov/compound/mexidol   

² “About the Preparation”. (2018). Mexidol.ru, available online from https://en.mexidol.ru/about-the-preparation [Accessed September 26, 2018]

³ “News”. (2018). Mexidol.ru, available online from https://en.mexidol.ru/ [Accessed September 26, 2018]

⁴ Zor'kina, A.V., Kostin, Y.V., Inchina, V.I. et al. (1998). Antioxidant and hypolipidemic properties of mexidol and emoxypine during prolonged immobilization stress. Pharm Chem J, 32: 231.

⁵ Loznikovaa, S.G., Sukhodolab, A.A., Shcharbinac, N.Y., Shcharbina, D.G. (2015). [Effect of magnesium, acetylsalicilic acid and emoxypine on aggregation of platelets]. (Article in Russian). Biofizika, 59(6):1108-12

⁶ Pashin, E.N., Shvedova, A.A. (1989). [The effect of the synthetic antioxidant emoxypine on the tonus of the coronary vessels]. Farmakol Toksikol, 52(5):17-9.

⁷ Chugunov, A.V., Kamchatnov, P.R., Mikhaĭlova, N.A. (2009). [Correction of free-radical oxidation as a pathogenetic approach to the treatment of acute ischemic stroke]. Zh Nevrol Psikhiatr Im S S Korsakova, 109(10 Suppl 2):65-8.