N-benzyl- and N-p-nitrobenzyl-N-norketobemidone, and N-p-fluorobenzyl- N-normetazocine have been synthesized and found to have equivalent or higher affinity for the (σ(i)-binding site than the previously described (+)-N- benzylnormetazocine. None of the examined compounds had significant affinity for the σ2-binding site and few had high affinity for μ-, δ-, and κ- opioid receptors. (-)-N-Benzyl-N-normetazocine displayed weak agonist- antagonist activity and (-)-N-benzylnoroxymorphone had one-tenth the antagonist activity of naloxone.
|Original language||English (US)|
|Number of pages||11|
|Journal||Medicinal Chemistry Research|
|State||Published - 1998|
ASJC Scopus subject areas
- Pharmacology, Toxicology and Pharmaceutics(all)
- Organic Chemistry