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Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(Cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective .mu. opioid receptor antagonist

✍ Scribed by Schmidhammer, Helmut; Burkard, Willy P.; Eggstein-Aeppli, Lislott; Smith, Colin F. C.

Book ID
118017114
Publisher
American Chemical Society
Year
1989
Tongue
English
Weight
553 KB
Volume
32
Category
Article
ISSN
0022-2623

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πŸ“œ SIMILAR VOLUMES

Tritium Labelling of Cyprodime ( = (β€”)-1
Tritium Labelling of Cyprodime ( = (β€”)-17-(Cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one), a ΞΌ Receptor-Selective Opioid Antagonist
✍ Ferenc Γ–tvΓΆs; GΓ©za TΓ³th; Helmut Schmidhammer πŸ“‚ Article πŸ“… 1992 πŸ› John Wiley and Sons 🌐 German βš– 169 KB

## Abstract The preparation of [1‐^3^H]cyprodime (2), which has a specific activity of 31.6 Ci/mmol was carried out by catalytic tritiodehalogenation of 1‐bromocyprodime (3). Bromination of cyprodime was performed by using chloroperoxidase, KBr, and H~2~O~2~.

Synthesis and Biological Evaluation of 1
Synthesis and Biological Evaluation of 14-Alkoxymorphinans Part 4 opioid agonists and partial opioid agonists in a series of N-(cyclobutylmethyl)-14-methoxymorphinan-6-ones
✍ Helmut Schmidhammer; Willy P. Burkard; Lislott Eggstein-Aeppli πŸ“‚ Article πŸ“… 1989 πŸ› John Wiley and Sons 🌐 German βš– 522 KB

The N-(cyclobutylmethy1)morphinans 12, 19, 20, 21, 27, and 29 and the N-(2-cyanoethyl) analogue 33 were prepared from different precursors. Pharmacological evaluation (e.g. opioid receptor binding assays, acetic-acid writhing test, hot-plate assay) points to a partial opioid agonism of compounds 12,