SAR of Benzomorphan Derivatives (Benzazocines)
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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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