SYNTHESIS, IN-VITRO, AND IN-VIVO ACTIVITY OF N-P-SUBSTITUTEDBENZYL- (-)- AND (-N-NORMETAZOCINES, (-)- AND (+)-N-NORMORPHINANS, N-NORKETOBEMIDONES, AND (-)-N-NOR-4,5-EPOXYMORPHINANS())

Authors
MAY EL JACOBSON AE MATTSON MV COOP A ACETO MD BOWMAN ER TRAYNOR JR WOODS JH HARRIS LS
Citation
El. May et al., SYNTHESIS, IN-VITRO, AND IN-VIVO ACTIVITY OF N-P-SUBSTITUTEDBENZYL- (-)- AND (-N-NORMETAZOCINES, (-)- AND (+)-N-NORMORPHINANS, N-NORKETOBEMIDONES, AND (-)-N-NOR-4,5-EPOXYMORPHINANS()), Medicinal chemistry research, 8(6), 1998, pp. 311-321
Citations number
34
Categorie Soggetti
Chemistry Medicinal
Journal title
Medicinal chemistry research → ACNP
ISSN journal
10542523
Volume
8
Issue
6
Year of publication
1998
Pages
311 - 321
Database
ISI
SICI code
1054-2523(1998)8:6<311:SIAIAO>2.0.ZU;2-H
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 sigma(1)-binding site than the previously desc ribed (+)-N-benzylnormetazocine. None of the examined compounds had si gnificant affinity for the sigma(2)-binding site and few had high affi nity for mu-, delta, and kappa-opioid receptors. (-)-N-Benzyl-N-normet azocine displayed weak agonist-antagonist activity and (-)-N-benzylnor oxymorphone had one-tenth the antagonist activity of naloxone.