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    Pagoclone molecular structure

    Pagoclone Stats & Data

    NPS DataHub
    MW407.9
    FormulaC23H22ClN3O2
    CAS133737-48-1
    IUPAC(3S)-2-(7-chloro-1,8-naphthyridin-2-yl)-3-(5-methyl-2-oxohexyl)-3H-isoindol-1-one
    SMILESCC(C)CCC(=O)CC1c2ccccc2C(=O)N1c1ccc2ccc(Cl)nc2n1
    InChIKeyHIUPRQPBWVEQJJ-IBGZPJMESA-N
    Others
    Psychoactive Class Depressant

    Pharmacology

    DrugBank
    State Solid

    Description

    Pagoclone is an anxiolytic drug from the cyclopyrrolone family, which is related to other more well known drugs such as the sleeping medication zopiclone. It is one of a relatively recently developed class of medicines known as the nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures.

    Mechanism of Action

    Pagoclone is a subtype-selective drug which binds primarily to the alpha2/alpha3 subtypes of the GABAA receptor which are responsible for the anti-anxiety effects of these kind of drugs, but has relatively little efficacy at the alpha1 subtype which produces the sedative and memory loss effects.

    Pharmacodynamics

    Pagoclone was originally developed as an anti-anxiety drug, but never commercialised. It is a partial agonist acting at GABAA receptors in the brain. In contrast to zopiclone, pagoclone produces anxiolytic effects with little or no sedative or amnestic actions at low doses.

    Indication

    For the potential treatment of panic and anxiety disorders.

    Tolerance & Pharmacokinetics

    drugs.wiki

    Tolerance Decay

    Full tolerance 3d Half tolerance 8d Baseline ~14d
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