Bemethyl

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Bemethyl
Bemethyl.svg
Clinical data
Trade namesMetaprot, Antihot, Bemitil, Bemithylum, Bemactor
Synonymsbemetil, bemithil, bemithyl, bemythyl, Metaproth, Metaprote, 2-benzilidazol-thioethyl, 2-ethylthiobenzimidazole hydrobromide, 2-ethylsulfanyl-1H-benzimidazole;hydrobromide
Routes of
administration
Oral as (tablets or capsules)
Legal status
Legal status
  • US: Unscheduled Not FDA approved
  • ℞-only (RU)
Identifiers
CAS Number
PubChem CID
ChemSpider
Chemical and physical data
FormulaC9H10N2S
Molar mass178.25 g·mol−1
3D model (JSmol)

Bemethyl, also commonly referred to in literature as bemitil, is a synthetic actoprotector which is also antihypoxant (combating conditions of hypoxia), antioxidant, and antimutagenic. Certified in Ukraine as a dietary supplement, bemethyl is commonly used in preparing for international competitions by Ukrainian national sport teams.[1] Bemethyl is formulated as a hydrobromide salt. Its parent compound is 2-ethylsulfanyl-1H-benzimidazole.[2]

Medical uses[edit]

Effects and benefits[edit]

Bemethyl is primarily classified as an actoprotector; a synthetic adaptogen with significant capacity to increase physical performance.[1]

Bemethyl also has a positive effect on metabolic processes, allowing adaptation to conditions causing frequent hypoxia, and the obtained effect is long-lasting and also occurs after the end of dosage.[3]

Bemethyl has been shown to preserve both physical and mental capacity in high-altitude, low-oxygen environments, particularly by its effect in helping control excess serum levels of cholesterol and bilirubin, which are known to have negative effects especially during adjustment to high-altitude environments.[4]

Bemethyl has also been shown to prevent permanent hearing loss and facilitate recovery of hearing after mine-explosion trauma, when treatment is initiated immediately after injury.[5]

Clinical research[edit]

Anti-mutagenic[edit]

In one study, bemethyl was shown to prevent the mutagenic effect of white asbestos in mice and in cultured human whole blood.[6]

A study using mice showed bemethyl to reduce mutatation induced by certain mutagenic drugs.[7]

Another study using cells from human donors showed Bemethyl to be anticlastogenic (able to minimize chromosome breakages).[8]

Pharmacology[edit]

Pharmacokinetics[edit]

Bemethyl resists metabolization and is long-lived, accumulating in tissues over course of treatment. In one study involving rats, long-term administration of Bemethyl was accompanied by a 1.38-fold increase in drug concentration in the brain, and a 1.68-fold increase in its concentration in skeletal muscles. [9]

History[edit]

Bemethyl was developed in the 1970s by the Department of Pharmacology of the St. Petersburg State Military Medical Academy under the direction of Professor Vladimir Vinogradov. Professor Vinogradov and his research team earned the USSR State Prize for this accomplishment.[1]

First used with Soviet cosmonaughts, Bemethyl was also used to prepare athletes of the USSR national team for the Moscow 1980 Olympic Games. In the 1990s, bemethyl saw use as a basic medicinal agent in many of the corps of the Soviet and Russian armies, including Soviet troops in Afghanistan, as bemethyl facilitated increased endurance for soldiers over long marches, as well as an enhanced work capacity and stability to hypoxia and high temperatures. Bemethyl was also used to enhance the physical and mental capacities of workers deployed in the wake of the 1986 Chernobyl disaster.[1]

Legal[edit]

As of 2018, bemethyl is now placed on the 2018 Monitoring Program of the U.S. Anti-Doping Agency to evaluate misuse in sport.[10] [11]

References[edit]

  1. ^ a b c d Oliynyk, Sergiy; Oh, Sei-Kwan (2012). "The Pharmacology of Actoprotectors: Practical Application for Improvement of Mental and Physical Performance". Biomolecules & Therapeutics. 20 (5): 446–456. doi:10.4062/biomolther.2012.20.5.446. ISSN 1976-9148. PMC 3762282.
  2. ^ "PubChem Compound Summary for CID 9816609 (Bemethyl)".
  3. ^ Zarubina IV1; Nurmanbetova FN; Shabanov PD (August 2005). "Bemithyl potentiates the antioxidant effect of intermittent hypoxic training" (140(2)): 190–193. PMID 16282998.
  4. ^ Mahnovsky, V. P. (2001), "Pharmacological Correction of the Human Functional State in High Altitude Conditions" (PDF), RTO-MP-062, Operational Medical Issues in Hypo- and Hyperbaric Conditions, Toronto, Canada: NATO Science and Technology Organization, pp. 6-1..6-15, doi:10.14339/RTO-MP-062, ADPO 11064
  5. ^ Salikhov, Dr. Khafis (2012-07-17). Challenges in Treating Combat Injuries. Xlibris Corporation. p. 299.
  6. ^ Daugel'-Dauge NO; Durnev AD; Kulakova AV; Velichkovskiĭ BT (1995). "Corpuscular mutagenesis and its prevention" (1): 29–38. PMID 7767114.
  7. ^ Seredenin SB; Bobkov IuG; Durnev AD; Dubovskaia OIu (1986). "Mutagenic and antimutagenic properties of bemitil" (102(7)): 76–79. PMID 3089347.
  8. ^ Arutyunyan RM; Sarkisyan TF; Oganesyan GG; Durnev AD (March 1994). "Comparative investigation of anticlastogenic effects in cell cultures of healthy donors and patients with nettle-rash" (320(4)): 335–341. PMID 7508559.
  9. ^ Sergeeva, S. A.; Gainetdinov, I. L. (2006). "Distribution of bemitil in organs and tissues of rats after single or repeated administration". 141: 596. doi:10.1007/s10517-006-0230-0. ISSN 1573-8221.
  10. ^ "Major Changes – 2018 WADA Prohibited List". U.S. Anti-Doping Agency. Retrieved December 10, 2017.
  11. ^ "Monitoring Program – 2018 WADA Prohibited List". U.S. Anti-Doping Agency. Retrieved December 10, 2017. The World Anti-Doping Code (Article 4.5) states: "WADA, in consultation with Signatories and governments, shall establish a monitoring program regarding substances which are not on the Prohibited List, but which WADA wishes to monitor in order to detect patterns of misuse in sport."