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newest 2023spec sheet7 rows
Afobazole is a genuinely obscure case from the West's perspective, a Russian-developed anxiolytic approved for clinical use back in 2005 that never crossed over into Western markets or Western awareness, despite being sold over the counter across Russia for two decades. Rather than working directly on GABA-A receptors like a benzodiazepine, it acts through the sigma-1 receptor chaperone system and restores the stress-desensitized GABA-benzodiazepine complex's normal sensitivity, a mechanism that in theory explains why it produces anxiolytic effects comparable to benzodiazepines in Russian trials without sedation or muscle relaxation. It sits in the archive mainly because it is a real, marketed, mechanistically distinct anxiolytic that almost nobody outside Russia and post-Soviet pharmacology literature has heard of.
- calm without the fog; no sedation or muscle slackening
- Russian trials rated it comparable to benzodiazepines
- works through sigma-1, not the benzodiazepine site
- approved and sold over the counter in Russia since 2005
- preclinical models show neuroprotection via sigma-1
- a real marketed anxiolytic the West simply never imported
- Afobazole has been sold over the counter in Russia since 2005, yet it barely appears in Western psychopharmacology textbooks or FDA drug databases.
Mechanism
Acts primarily as a sigma-1 receptor /chaperone modulator, with secondary activity at MAO-A and NQO2 (quinone reductase 2); rather than binding -A directly, it is thought to prevent stress-induced desensitization of the GABA-benzodiazepine receptor complex and restore its normal function.
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
Two decades of over-the-counter use in Russia have not produced a serious toxicity signal, and the reported adverse events are mild: headache that usually settles without stopping, plus occasional allergic reactions. Unlike a benzodiazepine it is not reported to cause sedation, muscle relaxation, tolerance or withdrawal. It is contraindicated in pregnancy and breastfeeding and in under-18s, and the tablets contain lactose. It potentiates carbamazepine's anticonvulsant and diazepam's anxiolytic effects. The honest gap is depth, not a known hazard: no FDA or EMA review, and safety data drawn mostly from small manufacturer-linked Russian trials.
History
Discovered and developed at the Zakusov Institute of Pharmacology (Russian Academy of Medical Sciences), Moscow; registered and marketed in Russia from 2006 as Afobazole; its sigma-1-centered mechanism was characterized in the years following clinical launch; never filed for Western regulatory approval.
Subjective profileweighing the evidence above
A real, marketed anxiolytic with a genuinely unusual sigma-1-based mechanism; obscure in the West mainly for geographic and regulatory reasons, not because it failed as a drug.
Where to buy
Suppliers
Vendors carrying Afobazole, with live product details and codes. Links are affiliate links that support the wiki at no cost to you.
RUPharma🌐
Afobazole
Research
- 2018first citedOn the Mechanism of the Cardioprotective Action of σ(1) Receptor Agonist Anxiolytic Fabomotizol…
- 2023most recentThe Effect of Original Russian Neurotropic Drugs on Organic Anion Transporting Polypeptides OAT…
- 1.Involvement of Chaperone Sigma1R in the Anxiolytic Effect of Fabomotizole
- 2.On the Mechanism of the Cardioprotective Action of σ(1) Receptor Agonist Anxiolytic Fabomotizole Hydrochloride (Afobazole).
- 3.The Effect of Original Russian Neurotropic Drugs on Organic Anion Transporting Polypeptides OATP1B1 and OATP1B3
3 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
Is afobazole the same as a benzodiazepine?
No. It does not bind GABA-A receptors directly the way benzodiazepines do; it works through sigma-1 receptor chaperone activity and is reported to lack the sedation and dependence risk of benzodiazepines.
Can you get afobazole outside Russia?
It has never been approved by the FDA or EMA, so it is not available through normal pharmacy channels in the US or EU; it remains a Russian OTC anxiolytic.
Limitations of the evidence
- limited Western safety data since it has never been through FDA/EMA review
- efficacy data comes almost entirely from Russian-language clinical literature, which is harder to independently verify