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    Amfecloral molecular structure

    Amfecloral Stats & Data

    Stimulant Research-chemical
    Acutran Amphecloral
    NPS DataHub
    MW264.58
    FormulaC11H12Cl3N
    CAS5581-35-1
    IUPAC2,2,2-trichloro-''N''-(1-phenylpropan-2-yl)ethanimine
    SMILESCC(N=CC(Cl)(Cl)Cl)Cc1ccccc1
    InChIKeyVBZDETYCYXPOAK-OVCLIPMQSA-N
    Phenethylamines; 2020/1. Von 2-Phenethylamin abgeleitete Verbindungen
    Chemical Class Amphetamine
    Psychoactive Class Stimulant
    Half-Life Parent compound ≈ 2–3 h; released amphetamine 9–14 h; trichloroethanol 4–8 h

    Pharmacology

    DrugBank
    State Solid

    Description

    Amfecloral is a stimulant drug of the phenethylamine and amphetamine chemical classes. For a short period of time, it was available under the brand Acutran and indicated as an appetite suppressant, but this product no longer exists. It acts as a prodrug which splits to form amphetamine and chloral hydrate, similarly to clobenzorex and related compounds, except that the N-substituent, in this case, yields a compound that is active in its own right. The chloral hydrate metabolite is a gabaminergic sedative/hypnotic, and would in theory counteract some of the stimulant effects of the amphetamine metabolite. This would produce an effect similar to the amphetamine/barbiturate combinations previously used in psychiatric medications.

    Indication

    Used as an appetite suppressant.

    Receptor Profile

    Receptor Actions

    Modulators
    GABA-A receptor positive allosteric modulator (from chloral hydrate/trichloroethanol metabolite)
    Other
    Dopamine-norepinephrine releasing agent (from amphetamine metabolite)

    Effect Profile

    Curated
    Stimulant 5.6

    Strong anxiety/jitters with moderate euphoria and focus, mild stimulation

    Stimulation / Energy×3
    5
    Euphoria / Mood Lift×2
    7
    Focus / Productivity×2
    7
    Anxiety / Jitters×1
    8
    Based on reports from:
    Erowid Experience Reports PsychonautWiki Amfecloral

    Tolerance & Pharmacokinetics

    drugs.wiki
    Half-Life
    Parent compound ≈ 2–3 h; released amphetamine 9–14 h; trichloroethanol 4–8 h
    Addiction Potential
    Moderate-to-high. Like other amphetamine prodrugs, repeated use can drive psychological dependence, sleep loss, and dysphoria on cessation. The chloral component can add tolerance/dependence to GABAergic sedatives with residual daytime somnolence after repeated dosing.

    Tolerance Decay

    Full tolerance 18d Half tolerance 5d Baseline ~42d

    Tolerance figures are extrapolated from general amphetamine patterns and chloral-hypnotic tolerance (which develops rapidly) rather than direct studies on amfecloral; treat as approximate and conservative. Avoid consecutive-day use; allow multi-day breaks to limit sleep disruption and crash severity.

    Cross-Tolerances

    Amphetamine
    50% ●○○
    Methamphetamine
    40% ●○○
    Other amphetamine prodrugs (e.g., clobenzorex)
    50% ●○○
    Cathinones
    30% ●○○
    Other GABAergic hypnotics (chloral/‘Z-drugs’/barbiturates)
    40% ●○○

    Harm Reduction

    drugs.wiki

    • Amfecloral is a Schiff-base (imine) prodrug that splits in vivo to amphetamine (stimulant) and chloral hydrate→trichloroethanol (sedative–hypnotic), which explains its smoother onset and biphasic profile. The chloral-derived metabolite positively modulates GABA-A and adds residual sedation; combining with other depressants (alcohol, benzos, opioids, barbiturates) can cause dangerous respiratory depression, especially as the stimulant wears off.

    • Amphetamine increases heart rate and blood pressure; hypertensive crises and severe toxicity can occur with MAOIs. Avoid MAOIs (including linezolid/methylene blue) and allow appropriate washouts. Monitor HR/BP and avoid if you have significant cardiovascular disease.

    • CYP2D6 status and inhibitors (fluoxetine, paroxetine, quinidine, bupropion, dronedarone) can raise amphetamine exposure; tramadol and dextromethorphan raise seizure/serotonin risks, especially with stimulants. Treat combinations as higher risk.

    • Because onset is slower than plain amphetamine, premature redosing can lead to stacking and delayed over-intoxication; wait 2–3 hours before any redose, and avoid chasing early. Amphetamine elimination is pH-dependent; antacids/alkalinizers can prolong effects and insomnia.

    • Authentic material is rare; the name is sometimes misused online. Prefer lab-based drug checking (FTIR/GC–MS) through reputable services; reagent tests may not be discriminative for this prodrug.

    • Avoid non-oral routes: the prodrug relies on hydrolysis and chloral/chloro-derivatives can irritate mucosa; non-oral pharmacokinetics are undocumented and may increase harm without benefit.

    • Do not drive or perform safety-critical tasks during the session or the following morning due to possible lingering sedation from the chloral metabolite. Residual somnolence is well documented with chloral hydrate.

    • If combining with any sedative for sleep, use the smallest effective dose with a sober sitter present; the stimulant may mask intoxication until it fades, at which point respiratory depression from depressants can emerge.

    References

    Data Sources

    Cited References

    Drugs.wiki References

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