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    Cinolazepam molecular structure

    Cinolazepam Stats & Data

    Geroderm
    NPS DataHub
    MW357.77
    FormulaC18H13ClFN3O2
    CAS75696-02-5
    IUPAC3-[7-chloro-5-(2-fluorophenyl)-3-hydroxy-2-oxo-3H-1,4-benzodiazepin-1-yl]propanenitrile
    SMILESN#CCCN1C(=O)C(O)N=C(c2ccccc2F)c2cc(Cl)ccc12
    InChIKeyXAXMYHMKTCNRRZ-UHFFFAOYSA-N
    Chemical Class Benzodiazepine
    Psychoactive Class Depressant

    Pharmacology

    DrugBank
    Half-life 9 hours State Solid Metabolism Hepatic.

    Description

    Cinolazepam is a benzodiazepine derivative with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant activity. It is not approved in Canada or America.

    Mechanism of Action

    Cinolazepam binds to central benzodiazepine receptors which interact allosterically with GABA receptors. This potentiates the effects of the inhibitory neurotransmitter GABA, increasing the inhibition of the ascending reticular activating system and blocking the cortical and limbic arousal that occurs following stimulation of the reticular pathways.

    Pharmacodynamics

    Cinolazepam is a benzodiazepine derivative with anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant activity. It is not approved in Canada or America.

    Absorption

    Bioavailability following oral administration is 90-100%.

    Toxicity

    The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma Grade I or Grade II following very large ingestions.

    Indication

    For the management of anxiety disorders or for the short-term relief of the symptoms of anxiety or anxiety associated with depressive symptoms.

    Effect Profile

    Curated
    Benzodiazepine 7.1

    Strong euphoria and anxiolysis with mild sedation and cognitive impairment

    Anxiolysis×3
    8
    Sedation / Relaxation×2
    5
    Motor / Cognitive Impairment×1
    4
    Euphoria / Mood Lift×1
    10

    Tolerance & Pharmacokinetics

    drugs.wiki

    Tolerance Decay

    Full tolerance 3d Half tolerance 37d Baseline ~60d
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