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    Bemethyl (bemitil) molecular structure

    Bemethyl (bemitil)

    NootropicsApproved (Russia)

    Also known as: Bemitil, Bemithyl, Metaprot, Bemactor, Antihot, 2-ethylthiobenzimidazole, 2-(ethylthio)benzimidazole hydrobromide

    Bemethyl, known in the Russian literature as bemitil and sold in the region under names including Metaprot, Bemactor and Antihot, is 2-ethylthiobenzimidazole, normally handled as the hydrobromide salt. It came out of work led by Vladimir Vinogradov at the Department of Pharmacology of the Military Medical Academy in Leningrad during the 1970s, which set out to define a class of drugs the authors called actoprotectors: agents that raise tolerance of physical work without raising oxygen consumption or heat production.

    Half-Life: Not established in humans; in healthy volunteers given a single 250 mg oral dose of the Metaprot capsule form, peak serum ethylthiobenzimidazole averaged 0.91 microg/mL at about 1.06 h, and no terminal half-life was reported (PMID: 21870773)Route: OralMW: 259.17 g/mol (hydrobromide salt); 178.26 g/mol (free base)CAS: 63513-71-3 (hydrobromide); 14610-11-8 (free base)
    Last reviewed:
    Nootropics
    Category
    Approved (Russia)
    Research Stage

    Overview

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    At A Glance

    Mechanism

    Bemethyl has no single identified receptor target. Reviews of the actoprotector class attribute its effects to a metabolic action: increased synthesis of RNA and of proteins, particularly gluconeogenesis enzymes in liver and kidney and mitochondrial enzymes, which supports lactat

    Half-Life
    Not established in humans; in healthy volunteers given a single 250 mg oral dose of the Metaprot capsule form, peak serum ethylthiobenzimidazole averaged 0.91 microg/mL at about 1.06 h, and no terminal half-life was reported (PMID: 21870773)
    Routes
    Oral
    Potential Benefits
    Increased maximal work performed and resistance to fatigue in mice under exhaustive load, with a profile different from the psychostimulant sydnocarb (PMID: 24009833)Cerebroprotective effect with normalized brain energy metabolism in rats after craniocerebral trauma, alone and combined with pyrazidol (PMID: 15514724)Hepatoprotective effect with reduced fibrosis in rats with experimental cirrhosis (PMID: 16845942)Potentiated the antioxidant adaptation produced by intermittent hypoxic training in rats (PMID: 16282998)Reduced lipid peroxidation and normalized liver enzyme values in rats poisoned with the organophosphate carbophos (PMID: 23012992)

    Overview

    Bemethyl, known in the Russian literature as bemitil and sold in the region under names including Metaprot, Bemactor and Antihot, is 2-ethylthiobenzimidazole, normally handled as the hydrobromide salt. It came out of work led by Vladimir Vinogradov at the Department of Pharmacology of the Military Medical Academy in Leningrad during the 1970s, which set out to define a class of drugs the authors called actoprotectors: agents that raise tolerance of physical work without raising oxygen consumption or heat production. Bemethyl was the first and remains the reference member of that class. It was given to Soviet cosmonauts, used in preparing athletes for the 1980 Moscow Olympic Games and issued widely in the Soviet armed forces, and after 1991 its official manufacture stopped in Russia before production resumed in Ukraine (PMID: 24009833). It was later re-registered in Russia as the capsule medicine Metaprot (marketing authorization holder AnviLab, manufacturer Farmproekt, product instruction approved 2014), indicated for restoring working capacity and for asthenia after infection, surgery or head injury (Russian State Register of Medicines, Metaprot). The proposed mechanism is metabolic rather than receptor based. Reviews describe increased synthesis of RNA and protein, particularly gluconeogenesis enzymes in liver and kidney and mitochondrial enzymes, which supports reuse of lactate and maintenance of ATP production under load, along with an indirect antioxidant effect through induction of antioxidant enzymes rather than direct radical scavenging. The authors of that review state plainly that the specific mechanism behind the protein expression effect remains unknown (PMID: 24009833). Animal work is extensive and almost all Russian. In rats, bemethyl distributed into liver, brain, kidney, spleen, heart, skeletal muscle, lung, adipose tissue and testes after single and repeated oral administration, accumulating most in liver (PMID: 17181062). It produced a cerebroprotective effect and normalized brain energy metabolism in rats after craniocerebral trauma (PMID: 15514724), a hepatoprotective effect with reduced fibrosis in rats with experimental cirrhosis (PMID: 16845942), and it strengthened the antioxidant adaptation produced by intermittent hypoxic training in rats (PMID: 16282998). Rat metabolism was mapped in 2021, with nine metabolites identified in 24 h urine after a single oral dose of 330 mg/kg and a benzimidazole-acetylcysteine conjugate as the most abundant (PMID: 34445727). Human data are thin by modern standards. A pharmacokinetic study in healthy volunteers given a single 250 mg oral dose reported a mean peak serum concentration of 0.91 microg/mL at about 1.06 h (PMID: 21870773). Clinical reports cover small groups: 15 patients with systemic lupus erythematosus (PMID: 10572751), seven children with epilepsy (PMID: 9324390) and patients with asthenic syndromes after moderate brain injury (PMID: 16404942). No large randomized placebo-controlled trial appears in the indexed English-language literature. Regulatory reality matters here. Bemethyl has no FDA or EMA authorization. In Ukraine it has been certified as a dietary supplement rather than a medicine, while in Russia it is registered as the medicine Metaprot (PMID: 24009833, PMID: 21870773). The World Anti-Doping Agency placed 2-ethylsulfanyl-1H-benzimidazole on its Monitoring Program from 2018 to 2021 and removed it for 2022, so it is on neither the current Prohibited List nor the Monitoring Program; an excretion study in six volunteers showed the parent drug and its glucuronide stay detectable in urine for weeks (PMID: 30346653). What is sold online as a bemethyl solution is a research chemical rather than the capsule product used in the published studies, and nothing verifies its identity or content.

    Potential Research Fields

    Actoprotectors and adaptogensExercise physiologyAntihypoxantsAnti-doping analysis

    Chemical Information

    IUPAC Name

    Not yet available

    CAS Number

    63513-71-3 (hydrobromide); 14610-11-8 (free base)

    Molecular Formula

    C9H11BrN2S (hydrobromide); C9H10N2S (free base)

    Molecular Mass

    259.17 g/mol (hydrobromide salt)

    Dosing & Protocols

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    Interactions

    Contraindications

    Reported contraindications in the Russian clinical literature are hypoglycemia and concurrent barbiturate treatment (PMID: 24009833). Mechanism-based caution applies to drugs cleared by cytochrome P450, since bemethyl acted as a mixed-type P450 inducer in rat liver and altered monooxygenase activity in human lymphocytes in vitro (PMID: 12227093). Not studied in human pregnancy; the one rat study found lower post-implantation loss, higher fetal weight and faster reflex maturation rather than harm (PMID: 17402591). The Russian Metaprot label lists severe hepatic dysfunction, epilepsy, hypertension, glaucoma, coronary disease, arrhythmias, pregnancy and lactation as contraindications.

    Research Disclaimer

    This interaction data is compiled from published research and community reports. It may not be exhaustive. Always consult a healthcare professional before combining compounds.

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    9-Me-BC (9-Methyl-β-carboline)

    NootropicsPreclinical

    9-Methyl--carboline (9-Me-BC) is a synthetic -carboline alkaloid that has drawn nootropic-community interest for a preclinical property that is genuinely unusual among -carbolines: in rodent and cell-culture studies it appears to stimulate the dopaminergic phenotype - raising tyrosine hydroxylase, the number of differentiated dopamine neurons and dopamine content - while also showing neuroprotective, neurorestorative and anti-inflammatory effects, plus in-vitro MAO-A/MAO-B inhibition [PMID:17913302, PMID:20374418, PMID:32285253].

    t½ Not characterized in humans (no pharmacokinetic data). Community/anecdotal only: ~5-25 mg per day, oral. No validated or approved human dose exists.
    6 studiesView Profile

    Aniracetam

    NootropicsApproved (Italy)

    Aniracetam is a pyrrolidinone in the racetam family, developed by Hoffmann-La Roche under the code Ro 13-5057.

    t½ About half an hour for the parent drug in humans. Plasma elimination half-life was 0.47 to 0.49 hours after a single 400 mg oral dose in 20 healthy male volunteers (PMID: 19025058). Aniracetam is extensively metabolized to N-anisoyl-GABA and anisic acid; in six elderly hospitalized patients with cerebrovascular disease and reduced creatinine clearance, metabolite half-life was 4 to 7 times longer than in young volunteers (PMID: 9062694).
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    Bromantane

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    t½ Not characterized in humans. Dihexa was engineered for metabolic stability (resistant to plasma and enzymatic degradation) and blood-brain-barrier penetration; in preclinical work its central procognitive effects appear to outlast its plasma presence. 5 to 40 mg oral per day (anecdotal range; no established human dose)
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    t½ Mean terminal half-life 4.82 hours, range 4.06 to 6.99 hours, after single oral doses in adolescents aged 12 to 17, with the drug excreted for the most part unchanged through the kidneys (PMID: 29339723). After intravenous dosing in animals, elimination half-life was 0.67 hours in rats, 2.1 hours in dogs and 1.3 hours in monkeys, with high systemic availability after oral dosing in all three species (PMID: 10604039).
    PreclinicalView Profile

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    Research Score

    30

    0 PubMed studies

    Quality Indicators

    Data Completeness

    63%
    Description
    Mechanism of Action
    Chemical Data
    Dosing Protocols
    Safety Profile
    PubMed Studies
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    Vendor Listings

    Quick Facts

    Half-Life

    Not established in humans; in healthy volunteers given a single 250 mg oral dose of the Metaprot capsule form, peak serum ethylthiobenzimidazole averaged 0.91 microg/mL at about 1.06 h, and no terminal half-life was reported (PMID: 21870773)

    Molecular Weight

    259.17 g/mol (hydrobromide salt)

    Administration

    Oral

    CAS Number

    63513-71-3 (hydrobromide); 14610-11-8 (free base)

    Trial Phase

    Approved (Russia)

    0

    Research Disclaimer

    This information is for educational and research purposes only. Not intended as medical advice. Consult a healthcare professional before use.

    Frequently Asked Questions

    What is Bemethyl (bemitil) used for in research?

    Bemethyl, known in the Russian literature as bemitil and sold in the region under names including Metaprot, Bemactor and Antihot, is 2-ethylthiobenzimidazole, normally handled as the hydrobromide salt. It came out of work led by Vladimir Vinogradov at the Department of Pharmacology of the Military Medical Academy in Leningrad during the 1970s, which set out to define a class of drugs the authors called actoprotectors: agents that raise tolerance of physical work without raising oxygen consumption or heat production. Bemethyl was the first and remains the reference member of that class. It was given to Soviet cosmonauts, used in preparing athletes for the 1980 Moscow Olympic Games and issued widely in the Soviet armed forces, and after 1991 its official manufacture stopped in Russia before production resumed in Ukraine (PMID: 24009833). It was later re-registered in Russia as the capsule medicine Metaprot (marketing authorization holder AnviLab, manufacturer Farmproekt, product instruction approved 2014), indicated for restoring working capacity and for asthenia after infection, surgery or head injury (Russian State Register of Medicines, Metaprot).

    The proposed mechanism is metabolic rather than receptor based. Reviews describe increased synthesis of RNA and protein, particularly gluconeogenesis enzymes in liver and kidney and mitochondrial enzymes, which supports reuse of lactate and maintenance of ATP production under load, along with an indirect antioxidant effect through induction of antioxidant enzymes rather than direct radical scavenging. The authors of that review state plainly that the specific mechanism behind the protein expression effect remains unknown (PMID: 24009833).

    Animal work is extensive and almost all Russian. In rats, bemethyl distributed into liver, brain, kidney, spleen, heart, skeletal muscle, lung, adipose tissue and testes after single and repeated oral administration, accumulating most in liver (PMID: 17181062). It produced a cerebroprotective effect and normalized brain energy metabolism in rats after craniocerebral trauma (PMID: 15514724), a hepatoprotective effect with reduced fibrosis in rats with experimental cirrhosis (PMID: 16845942), and it strengthened the antioxidant adaptation produced by intermittent hypoxic training in rats (PMID: 16282998). Rat metabolism was mapped in 2021, with nine metabolites identified in 24 h urine after a single oral dose of 330 mg/kg and a benzimidazole-acetylcysteine conjugate as the most abundant (PMID: 34445727).

    Human data are thin by modern standards. A pharmacokinetic study in healthy volunteers given a single 250 mg oral dose reported a mean peak serum concentration of 0.91 microg/mL at about 1.06 h (PMID: 21870773). Clinical reports cover small groups: 15 patients with systemic lupus erythematosus (PMID: 10572751), seven children with epilepsy (PMID: 9324390) and patients with asthenic syndromes after moderate brain injury (PMID: 16404942). No large randomized placebo-controlled trial appears in the indexed English-language literature.

    Regulatory reality matters here. Bemethyl has no FDA or EMA authorization. In Ukraine it has been certified as a dietary supplement rather than a medicine, while in Russia it is registered as the medicine Metaprot (PMID: 24009833, PMID: 21870773). The World Anti-Doping Agency placed 2-ethylsulfanyl-1H-benzimidazole on its Monitoring Program from 2018 to 2021 and removed it for 2022, so it is on neither the current Prohibited List nor the Monitoring Program; an excretion study in six volunteers showed the parent drug and its glucuronide stay detectable in urine for weeks (PMID: 30346653). What is sold online as a bemethyl solution is a research chemical rather than the capsule product used in the published studies, and nothing verifies its identity or content.

    What forms does Bemethyl (bemitil) come in?

    Bemethyl (bemitil) is available in liquid form.

    How much does Bemethyl (bemitil) cost?

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    Research Tools

    Related Compounds

    View All

    9-Me-BC (9-Methyl-β-carboline)

    NootropicsPreclinical

    9-Methyl--carboline (9-Me-BC) is a synthetic -carboline alkaloid that has drawn nootropic-community interest for a preclinical property that is genuinely unusual among -carbolines: in rodent and cell-culture studies it appears to stimulate the dopaminergic phenotype - raising tyrosine hydroxylase, the number of differentiated dopamine neurons and dopamine content - while also showing neuroprotective, neurorestorative and anti-inflammatory effects, plus in-vitro MAO-A/MAO-B inhibition [PMID:17913302, PMID:20374418, PMID:32285253].

    t½ Not characterized in humans (no pharmacokinetic data). Community/anecdotal only: ~5-25 mg per day, oral. No validated or approved human dose exists.
    6 studiesView Profile

    Aniracetam

    NootropicsApproved (Italy)

    Aniracetam is a pyrrolidinone in the racetam family, developed by Hoffmann-La Roche under the code Ro 13-5057.

    t½ About half an hour for the parent drug in humans. Plasma elimination half-life was 0.47 to 0.49 hours after a single 400 mg oral dose in 20 healthy male volunteers (PMID: 19025058). Aniracetam is extensively metabolized to N-anisoyl-GABA and anisic acid; in six elderly hospitalized patients with cerebrovascular disease and reduced creatinine clearance, metabolite half-life was 4 to 7 times longer than in young volunteers (PMID: 9062694).
    PreclinicalView Profile

    Bromantane

    NootropicsRussia Approved

    Bromantane is an atypical psychostimulant and anxiolytic developed in the 1980s at the Zakusov Institute of Pharmacology of the Russian Academy of Medical Sciences, originally created as an adaptogen for Soviet military and elite athletic use and later approved in Russia for the treatment of neurasthenic and asthenic disorders under the trade name Ladasten.

    34 studiesView Profile

    Cyclazodone

    NootropicsPreclinical

    Cyclazodone is the N-cyclopropyl derivative of pemoline, a 4-oxazolidinone stimulant.

    PreclinicalView Profile

    Dihexa

    NootropicsPreclinical

    Dihexa is a synthetic peptide analogue of the angiotensin IV metabolite LVV-hemorphin-7, developed at Washington State University.

    t½ Not characterized in humans. Dihexa was engineered for metabolic stability (resistant to plasma and enzymatic degradation) and blood-brain-barrier penetration; in preclinical work its central procognitive effects appear to outlast its plasma presence. 5 to 40 mg oral per day (anecdotal range; no established human dose)
    1 studiesView Profile

    Fasoracetam (NS-105)

    NootropicsPhase 2

    Fasoracetam is a racetam developed by Nippon Shinyaku in Japan under the code NS-105 and taken into clinical development for vascular dementia.

    t½ Mean terminal half-life 4.82 hours, range 4.06 to 6.99 hours, after single oral doses in adolescents aged 12 to 17, with the drug excreted for the most part unchanged through the kidneys (PMID: 29339723). After intravenous dosing in animals, elimination half-life was 0.67 hours in rats, 2.1 hours in dogs and 1.3 hours in monkeys, with high systemic availability after oral dosing in all three species (PMID: 10604039).
    PreclinicalView Profile

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