SYNTHESIS AND BIOLOGICAL EVALUATION OF 14-ALKOXYMORPHINANS - PART 15 - NOVEL DELTA-OPIOID RECEPTOR ANTAGONISTS WITH HIGH-AFFINITY AND SELECTIVITY IN THE 14-ALKOXY-SUBSTITUTED INDOLOMORPHINAN SERIES
H. Schmidhammer et al., SYNTHESIS AND BIOLOGICAL EVALUATION OF 14-ALKOXYMORPHINANS - PART 15 - NOVEL DELTA-OPIOID RECEPTOR ANTAGONISTS WITH HIGH-AFFINITY AND SELECTIVITY IN THE 14-ALKOXY-SUBSTITUTED INDOLOMORPHINAN SERIES, Helvetica Chimica Acta, 81(6), 1998, pp. 1064-1069
The indolomorphinans 4-7 were prepared from their corresponding morphi
nan-6-one derivatives 8-11 via Fischer indole synthesis. Compounds 4 a
nd 5 exhibited higher antagonist potency at delta opioid receptors in
the mouse vas deferens preparation than the reference drug HS 378 (2),
while compounds 6 and 7 were less potent.