What Is The Pharmacophore Of Paracetamol?

I’m working on a Grade 12 Chemistry assignment about paracetamol and I’m struggling to understand just how it relieves pain. I am aware that no one really knows how it works and that there are multiple theories, however, I am working with the one that states that it inhibits the COX-3 enzyme. If it does in fact inhibit COX-3, then how does it do it? What is the pharmacophore of paracetamol?.

3 thoughts to “What Is The Pharmacophore Of Paracetamol?”

  1. Sup Chris Johnson aha,
    dude im totally lost about it too, basically from what i have found is that it is the amide component of paracetamol that contributes to the reaction in the brain and the entailing analgesic effect. according to a pharmacist i asked, either the OH or NH directly leading off the benzene ring oxidises the most easiest and so would be more inclined to react with receptors in the brain.
    U O ME.

  2. Acetaminophen apparently inhibits COX activity by reducing the oxidized form of the enzyme back to the catalytically inactive resting state and this occurs more readily when the enzyme activity and consequently the peroxide tone are low. This is most easily accomplished by the NH group. So, if you had to speculate as to the pharmacophore, you mihgt suggest it to be the amine.

  3. Acetaminophen is a central inhibitor of Cycolooxyenase metabolism of Arachidonic Acid (20 Carbon molecule). Which substype it has more affinity toward, I simply don’t know. The pharmocokinetics/dynamice can be found by simply looking in any packet or in a text of Pharmaceuticals.
    Good luck

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