Home
    Disclaimer
    Gaboxadol molecular structure

    Gaboxadol Stats & Data

    Thip Ov101 Mk-0928 Lu-2-030 Lu-02-030
    Chemical Class Benzodiazepine
    Psychoactive Class Depressant
    Half-Life Short-acting. Publicly accessible summaries do not provide definitive human half-life; treat as short duration with potentially longer functional impairment after sleep.

    Pharmacology

    DrugBank
    State Solid

    Description

    Gaboxadol also known as 4,5,6,7-tetrahydroisoxazolo(5,4-c)pyridin-3-ol (THIP) is an experimental sleep aid drug developed by Lundbeck and Merck, who reported increased deep sleep without the reinforcing effects of benzodiazepines. Development of Gaboxadol was stopped in March 2007 after concerns regarding safety and efficacy. It acts on the GABA system, but in a seemingly different way from benzodiazepines and other sedatives.

    Indication

    Investigated for use/treatment in sleep disorders and insomnia.

    Effect Profile

    Curated + 2 Reports
    Benzodiazepine 4.3

    Strong cognitive impairment with mild anxiolysis, sedation, and euphoria

    Anxiolysis×3
    5
    Sedation / Relaxation×2
    5
    Motor / Cognitive Impairment×1
    9
    Euphoria / Mood Lift×1
    4

    Tolerance & Pharmacokinetics

    drugs.wiki
    Half-Life
    Short-acting. Publicly accessible summaries do not provide definitive human half-life; treat as short duration with potentially longer functional impairment after sleep.
    Addiction Potential
    Low to moderate; limited reinforcing properties compared with benzodiazepines, but physiological dependence and tolerance are plausible with frequent use as with other GABAergic sedatives.

    Tolerance Decay

    Full tolerance 3d Half tolerance 7d Baseline ~14d

    Evidence on tolerance kinetics in humans is sparse. Rapid tolerance is expected with daily use by analogy to other GABAergic sedatives; some animal data suggest distinct receptor populations (extrasynaptic δ vs. synaptic γ2) which may alter cross-tolerance magnitude relative to benzodiazepines.

    Cross-Tolerances

    Benzodiazepines (GABA-A positive allosteric modulators)
    30% ●○○
    Barbiturates
    30% ●○○
    Z-drugs (zolpidem, zopiclone)
    30% ●○○

    Experience Report Analysis

    Erowid
    2 Reports
    2020–2021 Date Range
    2 With Age Data

    Demographics

    Gender Distribution

    Age Distribution

    Reports Over Time

    Harm Reduction

    drugs.wiki

    Gaboxadol is a direct-acting orthosteric GABA-A agonist that preferentially engages extrasynaptic δ-subunit–containing receptors mediating tonic inhibition; this explains deep sedation with less 'benzo-like' disinhibition and has implications for combinations and reversal strategies. Because it does not act at the benzodiazepine site, flumazenil is unlikely to reverse isolated gaboxadol intoxication; management is supportive with airway monitoring, especially if other depressants were involved. High or repeated doses have been associated anecdotally and in development reports with delirium, hallucinations, and amnesia; therefore, avoid pushing beyond the common range and do not stack redoses in one night. Combination with opioids, alcohol, GHB/GBL, benzodiazepines or Z-drugs substantially increases risk for respiratory depression, loss of consciousness, and aspiration; treat these combinations as high-risk and keep doses markedly lower if abstinence from mixing is not maintained. A structural study confirms binding at α4β3δ extrasynaptic GABA-A receptors, providing mechanistic support for potent slow-wave sleep promotion and pronounced motor incoordination; practice 'safe sleep' (no baths, hazards, or tasks) and plan not to drive until fully recovered. User reports indicate variability in time to peak and next-morning grogginess; if experimenting, take the first dose on a quiet night with supervision available and no next-day obligations. A harm-reduction lab warning has identified mis-sold material contaminated with ibotenic acid (an excitotoxic Amanita alkaloid); obtain from trusted sources, consider analytical testing where available, and do not consume products of uncertain identity. Start with an allergy test (~1 mg), then space trials by several days to gauge sensitivity and tolerance build-up; tolerance to GABAergic sedatives often develops quickly and resolves slowly. As with other strong sedatives, people with sleep apnea, chronic lung disease, or unstable cardiovascular disease are at higher risk from nocturnal hypoventilation; these groups should avoid use.

    ← Back to Gaboxadol