Synthesis and Biological Evaluation of 14‐Alkoxymorphinans, V1): 6‐Deoxocyprodime, an Opioid Antagonist with Decreased μ Receptor Selectivity in Comparison to Cyprodime
- 1 January 1991
- journal article
- research article
- Published by Wiley in Archiv der Pharmazie
- Vol. 324 (4) , 209-211
- https://doi.org/10.1002/ardp.19913240404
Abstract
N-Cyclopropylmethyl-4,14-dimethoxymorphinan (4) and N-cyclopropylmethyl-4-hydroxy-14-methoxymorphinan (5) have been prepared from cyprodime (1) by Wolff-Kishner reduction. Pharmacological studies (mouse vas deferens and guinea pig ileum preparations) revealed that there was no significant decrease of 4 in antagonist activity but in mu selectivity when compared with 1. The phenol 5 showed partial agonism at mu, kappa and delta receptors.Keywords
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