Flutoprazepam

CAS Number 25967-29-7
Molecular Formula C₁₉H₁₆ClFN₂O
Molecular Weight 342.8 g/mol
Purity ≥99.0%
Appearance White powder

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Product Description

Flutoprazepam is a potent benzodiazepine drug exhibits strong sedative, hypnotic, anxiolytic, anticonvulsant, and muscle relaxant properties, making it approximately four times more potent than diazepam (Valium) by weight. Its effects are long-lasting due to its active metabolite, N-desalkylflurazepam, which has a very long half-life of 40–250 hours and can be detected in the bloodstream for up to four days. In an experiment, 2 mg of flutoprazepam was administered to eight subjects, and while the parent compound was undetectable after nine hours, its metabolite N-desalkylflurazepam had a much greater concentration, with an average elimination half-life of 90 hours. Flutoprazepam is currently unregulated in most countries, although its parent compounds are classified as Schedule IV drugs under the 1971 United Nations Convention on Psychotropic Substances, which aimed to control the use of psychoactive substances.

Basic Information

  • IUPAC Name: 7-chloro-5-(o-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one

  • Other Names: Restas, KB-509

Uses

  • Primary Uses:

    • Severe insomnia

    • Anxiety disorders

    • Historically used for stomach ulcers due to muscle relaxant properties

  • Research Use: Primarily a research chemical or designer drug

  • Regional Use: Mainly used in Japan under the brand name Restas

Legal / Status

  • Regulation: Not approved for medical use in most countries, including the United States and the European Union

  • Controlled Substance: Classified as a controlled substance in many countries

  • International Convention: Not listed under the 1971 Convention on Psychotropic Substances

Side Effects

  • Common Side Effects:

    • Drowsiness/sedation

    • Daytime sleepiness

    • Dizziness or lightheadedness

    • Cognitive impairment (memory problems, difficulty concentrating)

    • Muscle weakness

  • Serious Side Effects:

    • Risk of dependence and addiction with long-term use

    • Paradoxical reactions (agitation, anxiety, aggression)

    • Complex sleep behaviors (e.g., sleep-driving, sleep-walking)

Risks and Dangers

  • Dependence and Addiction: High potential for physical and psychological dependence

  • Tolerance: Users may need to increase the dose over time

  • Withdrawal Syndrome: Severe and potentially life-threatening symptoms

  • Overdose Risk: Increased when mixed with other CNS depressants (alcohol, opioids)

  • Cognitive Impairment: Significant drowsiness, confusion, memory problems

  • Lack of Quality Control: Unregulated status leads to risks of accidental overdose

Physical and Chemical Properties

  • Density: 1.37 g/cm³

  • Boiling Point: 539.3°C

  • Flash Point: 279.9°C

  • Solubility:

    • DMF: 30 mg/ml

    • DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml

    • DMSO: 25 mg/ml

    • Ethanol: 1 mg/ml

Structure

  • Chemical Family: 1,4-Benzodiazepine

  • Substitutions: Chloro (Cl) and fluoro (F) atoms

  • Core Scaffold: Benzodiazepinone with a phenyl substituent at the 5-position

  • Structure: 7-Chloro-1-(cyclopropylmethyl)-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepin-2-one

Pharmacology

  • Mechanism of Action: Acts as a GABA-A receptor positive allosteric modulator, enhancing the effect of GABA in the CNS.

  • Primary Effects: Sedative, hypnotic, anxiolytic, anticonvulsant, muscle relaxant

  • Potency: Approximately four times more potent than diazepam (Valium) by weight

  • Duration of Action: Long-lasting due to the active metabolite N-desalkylflurazepam

  • Metabolite: N-desalkylflurazepam (half-life: 40-250 hours)

Safety and Handling

  • Storage: Store according to product insert instructions

  • Handling: Follow usual precautionary measures for handling chemicals

  • Protective Equipment:

    • Breathing equipment: Not required

    • Hand protection: Use impermeable and resistant gloves

    • Eye protection: Not required

Ecological Information

  • Toxicity: No specific data available

  • Persistence and Degradability: No specific data available

  • Bioaccumulative Potential: No specific data available

  • Mobility in Soil: No specific data available

  • Water Hazard Class: 1 (slightly hazardous for water)

Disposal

  • Waste Treatment: Smaller quantities can be disposed of with household waste

  • Uncleaned Packagings: Dispose according to official regulations

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