Substance:Alpravalzafone

Alpravalzafone is a water-soluble prodrug of what is currently to be assumed Alprazolam.

Chemical structure of Alpravalzafone (Without regards to geometry)

It recently surfaced as a designer drug in Germany which is adjacent in its design to the Japanese benzodiazepine prodrug Rilmazafone. Little is known about the exact metabolites of this prodrug so far, but preliminary reports by users have demonstrated the presence of metabolites found in users of other common benzodiazepines. The report included detectable levels of Oxazepam, Hydroxy-Alprazolam (an Alprazolam metabolite) and Alprazolam. It is hereby unclear why the report includes the metabolite Oxazepam, as Alpravalzafone cannot metabolize into Oxazepam under normal conditions due to the addition of a triazolo group (the pentyl ring containing three nitrogens at the very top of the molecule), so contamination by the vendor or cross-contamination from other drugs may be possible here.

It is therefore assumed that the drug undergoes metabolism to Alprazolam in the blood in a similar fashion as Rilmazafone would, closing the open ring to form the diazepine structure. The compound was described in scientific literature by Aipsin (A Russian anti-narcotics company) as early as March of 2026, turning up in the first RC Vendor's stores shortly thereafter.

Dosage

The exact active dose is unclear, however, assuming full metabolism of the prodrug in the bloodstream, comparing the molecular weights, we can estimate that roughly 64% of the prodrug gets converted to Alprazolam.

Alprazolam's molecular weight: 308.77 g/mol Alpravalzafone's molecular weight: 482.38g/mol

Therefore: 308.77/482.38 = 0.6400970189 ~ 64%

It is unclear what exactly the redundant metabolites of this prodrug are, so currently use is not advised.

Chemistry

Basic data: Formula: C₂₂H₂₅Cl₂N₅O₂ Molar mass: 462.38g/mol SMILES: NC(C(=O)NCC1=NN=C(N1C1=C(C=C(C=C1)Cl)C(C1=CC=CC=C1)=O)C)C(C)C Systemic IUPAC name: 2-amino-N-((4-(2-benzoyl-4-chlorophenyl)-5-methyl-4H-1,2,4-triazol-3-yl)methyl)-3-methylbutanamid

Solubility: According to a user on eve&rave.ch, the powdered version of Alpravalzafone is very soluble in a 37,5% ethanol in water solution. Please note that co-ingestion of benzodiazepines with larger amounts of ethanol may posses additional dangers.

In a test performed by the editor, Alpravalzafone completely dissolved in both descaled tap water as well as a 99,9% pure propylene glycol solution.

Legal status

Alpravalzafone is as of early May 2026 not a controlled substance in Germany, however, would fall under the restrictions imposed by the NpSG as soon as it enters non-acidic conditions and hydrolizes back into the closed ring form.

Alpravalzafone is not currently considered a controlled substance in Russia or Belarus.