Abstract
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) |
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Pages (from-to) | 311-321 |
Number of pages | 11 |
Journal | Medicinal Chemistry Research |
Volume | 8 |
Issue number | 6 |
State | Published - 1998 |
Externally published | Yes |
ASJC Scopus subject areas
- Pharmacology, Toxicology and Pharmaceutics(all)
- Organic Chemistry