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Antipsychotic
Desmethylclozapine
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    Desmethylclozapine

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    Desmethylclozapine
    Skeletal formula of desmethylclozapine
    Space-filling model of the desmethylclozapine molecule
    Clinical data
    Routes of
    administration    		 Oral
    ATC code
    • none
    Legal status
    Legal status
    • In general: uncontrolled
    Identifiers
    • 8-chloro-11-piperazin-1-yl-5H-dibenzo[b,e][1,4]diazepine
    CAS Number
    PubChem CID
    IUPHAR/BPS
    ChemSpider
    UNII
    ChEMBL
    CompTox Dashboard (EPA)
    ECHA InfoCard 100.164.220
    Chemical and physical data
    Formula C17H17ClN4
    Molar mass 312.80 g·mol−1
    3D model (JSmol)
    • Clc1ccc2Nc4ccccc4C(=N\c2c1)/N3CCNCC3

    N-Desmethylclozapine (NDMC), or norclozapine, is a major active metabolite of the atypical antipsychotic drug clozapine. Unlike clozapine, it possesses intrinsic activity at the D2/D3 receptors, and acts as a weak partial agonist at these sites similarly to aripiprazole and bifeprunox. Notably, NDMC has also been shown to act as a potent and efficacious agonist at the M1 and δ-opioid receptors, unlike clozapine as well. It was hypothesized that on account of these unique actions, NDMC might underlie the clinical superiority of clozapine over other antipsychotics. However, clinical trials found NMDC itself ineffective in the treatment of schizophrenia. This may be because it possesses relatively low D2/D3 occupancy compared to 5-HT2 (<15% versus 64-79% at a dose of 10–60 mg/kg s.c. in animal studies). Albeit not useful in the treatment of positive symptoms on its own, it cannot be ruled out that NDMC may contribute to the efficacy of clozapine on cognitive and/or negative symptoms.

    See also



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