Question:

When 6-OH of morphine is replaced by 6-O-acetyl group, then the activity will ___.

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Increased lipophilicity due to acetylation enhances blood-brain barrier penetration, increasing drug activity.
Updated On: Jun 16, 2025
  • increase
  • decrease
  • no effect
  • Antagonistic
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The Correct Option is A

Solution and Explanation

Replacing the 6-hydroxy group in morphine with a 6-O-acetyl group increases the lipophilicity of the molecule, enhancing its ability to cross the blood-brain barrier. This results in increased potency and activity of the molecule, as seen in compounds like heroin (diacetylmorphine).
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