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    Carfentanil Stats & Data

    Carfentanyl Wildnil R-33799 4-methoxycarbonylfentanyl
    PubChem
    MW394.5
    FormulaC24H30N2O3
    LogP3.8
    IUPACmethyl 1-(2-phenylethyl)-4-(N-propanoylanilino)piperidine-4-carboxylate
    InChIKeyYDSDEBIZUNNPOB-UHFFFAOYSA-N
    Chemical Class Anilidopiperidine
    Psychoactive Class Depressant
    Half-Life Unknown in humans; clinical management should assume potential for prolonged/rebound respiratory depression relative to heroin; extended observation advised in guidance for fentanyls.

    Measured Affinities

    Guide to PHARMACOLOGY

    Measured binding and functional data for carfentanil, curated by the IUPHAR/BPS Guide to PHARMACOLOGY. Each row cites the paper it came from. Lower concentrations mean tighter binding — a value in the sub-nanomolar range indicates a very potent interaction.

    Target Action Measure Value Concentration Species Source
    μ receptor Agonist pKi 10.62 0.024 nM Guinea pig PMID 1310142
    δ receptor Agonist pKi 8.48 3.31 nM Guinea pig PMID 1310142
    κ receptor Agonist pKi 7.37 42.66 nM Guinea pig PMID 1310142

    Reading this. pKi, pEC50 and pIC50 are negative log molar values, so a higher number means a tighter interaction; the concentration column converts them for you. Values from non-human species are laboratory measurements and do not translate directly to human effect. Receptor affinity is not a dose — it describes what a molecule binds, not how much of it is safe to take.

    Receptor data from the IUPHAR/BPS Guide to PHARMACOLOGY (v2026.2), licensed CC BY-SA 4.0. Matched to this substance by InChIKey.

    Effect Profile

    Curated
    Opioid 2.6

    Moderate sedation and itching/nausea with mild pain relief

    Euphoria / Warmth×3
    0
    Analgesia×2
    4
    Sedation / Relaxation×1
    7
    Itching / Nausea×1
    7

    Tolerance & Pharmacokinetics

    drugs.wiki
    Half-Life
    Unknown in humans; clinical management should assume potential for prolonged/rebound respiratory depression relative to heroin; extended observation advised in guidance for fentanyls.
    Addiction Potential
    Extremely high. Ultra‑potent µ‑opioid receptor agonist with severe overdose risk at microgram‑level exposures.

    Cross-Tolerances

    Fentanyl
    80% ●○○
    Morphine
    60% ●○○
    Other opioids
    50% ●○○

    Harm Reduction

    drugs.wiki

    Carfentanil is one of the most potent opioids identified in drug markets, with estimated quantitative potency around 10,000× morphine and ~100× fentanyl; human activity may begin at ~1 µg, but any specific human lethal dose remains unknown and likely varies widely with tolerance, route, and co‑ingestants. Treat any exposure as a medical emergency. Carfentanil has been detected as an adulterant or substitute for other opioids (e.g., heroin) and can appear in mixed drug supplies; users are often unaware of exposure. Overdose is characterized by rapid and profound respiratory depression, bradycardia, and loss of consciousness; naloxone can reverse opioid toxicity, but compared with heroin, fentanyl‑class overdoses may require faster administration, more rapid escalation, and overall higher or repeated doses of naloxone, with prolonged observation due to recurrent depression. Drug checking resources report that fentanyl test strips (FTS) can detect many fentanyl analogs, including carfentanil, but false negatives/positives are possible; pairing with confirmatory testing and careful sampling across a solution increases detection chances. Do not rely on a single negative result to assume safety. Polysubstance use—especially with benzodiazepines, alcohol, barbiturates, or gabapentinoids—markedly increases the risk of fatal respiratory depression and complicates reversal (naloxone does not reverse non‑opioid sedatives). Because of carfentanil’s potency and risk of recurrent toxicity, bystanders should call emergency services immediately, administer naloxone promptly (repeat if no response in 2–3 minutes), and provide rescue breathing until professionals take over. Expect need for multiple naloxone doses in some cases. Carfentanil presence in local markets is highly variable; relying on lab‑based drug checking programs (e.g., GC/MS) provides more definitive identification than immunoassay strips alone.

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