SAR of Benzomorphan Derivatives (Benzazocines)

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Chapter: Medicinal Chemistry : Narcotic Analgesics

Pentazocine produces analgesia because of its agonistic action on kappa opioid receptors. Pentazocine is a week antagonistic at μ receptors.


SAR of Benzomorphan Derivatives (Benzazocines)


  • Pentazocine produces analgesia because of its agonistic action on kappa opioid receptors. Pentazocine is a week antagonistic at μ receptors.

  • The trimethyl compound (R1 = R2 =CH3 ) is more active than dimethyl (R1=H, R2 = CH3 ) compound.

  • Placement of Nphenyl ethyl results in more activity than N-methyl compound.

  • Placement of methyl group in 9th position increases the activity. However -OH group decreases the activity.

  • N-allyl (or) N-cyclo proyl methyl group confers antagonistic activity. For example, Levallorphanol, Naloxone, and Naltreoxane.

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