SYNTHESIS AND BIOLOGICAL EVALUATION OF 14-ALKOXYMORPHINANS .12. A PHENETHYL ANALOG OF THE MU-SELECTIVE OPIOID RECEPTOR ANTAGONIST CYPRODIME

Authors
SCHMIDHAMMER H STANGL A FURST Z SZABO E BORSODI A PATEL D TRAYNOR JR
Citation
H. Schmidhammer et al., SYNTHESIS AND BIOLOGICAL EVALUATION OF 14-ALKOXYMORPHINANS .12. A PHENETHYL ANALOG OF THE MU-SELECTIVE OPIOID RECEPTOR ANTAGONIST CYPRODIME, Bioorganic & medicinal chemistry letters, 5(17), 1995, pp. 1923-1926
Citations number
15
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
17
Year of publication
1995
Pages
1923 - 1926
Database
ISI
SICI code
0960-894X(1995)5:17<1923:SABEO1>2.0.ZU;2-3
Abstract
The N-phenethyl analogue (compound 4) of the mu-selective opioid antag onist cyprodime (1) has been prepared and evaluated in radioligand bin ding, bioassays (guinea-pig ileum myenteric plexus and mouse vas defer ens preparations) and the rat tail flick test. It was found to possess remarkable affinity and high preference for mu opioid receptors and h igh antinociceptive potency which is comparable to its N-methyl analog ue 3.