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Mardepodect
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    Mardepodect

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    Mardepodect
    PF-2545920.svg
    Clinical data
    Other names PDF-2545920
    ATC code
    • None
    Legal status
    Legal status
    • Investigational
    Identifiers
    • 2-(4-(1-Methyl-4-pyridin-4-yl-1H-pyrazol-3-yl)phenoxymethyl)quinoline
    CAS Number
    PubChem CID
    DrugBank
    ChemSpider
    UNII
    KEGG
    ChEMBL
    Chemical and physical data
    Formula C25H20N4O
    Molar mass 392.462 g·mol−1
    3D model (JSmol)
    • n3c1ccccc1ccc3COc5ccc(cc5)-c2nn(C)cc2-c4ccncc4
    • InChI=1S/C25H20N4O/c1-29-16-23(18-12-14-26-15-13-18)25(28-29)20-7-10-22(11-8-20)30-17-21-9-6-19-4-2-3-5-24(19)27-21/h2-16H,17H2,1H3 ☒N
    • Key:AZEXWHKOMMASPA-UHFFFAOYSA-N ☒N
     ☒NcheckY (what is this?)  (verify)

    Mardepodect (developmental code name PF-2545920) is a drug which was developed by Pfizer for the treatment of schizophrenia. It acts as a phosphodiesterase inhibitor selective for the PDE10A subtype. The PDE10A enzyme is expressed primarily in the brain, mostly in the striatum, nucleus accumbens and olfactory tubercle, and is thought to be particularly important in regulating the activity of dopamine-sensitive medium spiny neurons in the striatum which are known to be targets of conventional antipsychotic drugs. Older PDE10A inhibitors such as papaverine have been shown to produce antipsychotic effects in animal models, and more potent and selective PDE10A inhibitors are a current area of research for novel antipsychotic drugs which act through a different pathway to conventional dopamine or 5-HT2A antagonist drugs and may have a more favourable side effects profile. Mardepodect is currently one of the furthest advanced PDE10A inhibitors in development and has progressed through to Phase II clinical trials in humans. In 2017, development of mardepodect for the treatment of schizophrenia and Huntington's disease was discontinued.


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