COMT inhibitor

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    COMT inhibitor - Presentation Transcript

    1. Increase the degree of activity
      Single benzene ring,
      Metabolized easier
      E
      Greatly reduce the O-methylation of the catechol hydroxyl group
      Entacapone
    2. E
      ntacapone
      Nitro group-electron withdrawing, stabilize the ionized catechol-COMT complex
      Entacapone @$#^88…
      Greatly reduce the extent of O-methylation of the catechol hydroxyl group
      More active than Tolcapone-ethyl group
      Entacapone
    3. Nitro group, stabilizing the ionized catechol-COMT complex
      Tolcapone
      Difficult to be metabolized,
      increase toxicity
      2 benzene ring, extend level of toxicity
      Responsible for the degree of activity
      Electron withdrawing,
      Strongly stabilized the ionized catechol-COMT complex

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