Paper
Synthesis and biological evaluation of 14-alkoxymorphinans. 2. (-)-N-(cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one, a selective mu opioid receptor antagonist.
Published Feb 1, 1989 · H. Schmidhammer, W. Burkard, L. Eggstein-Aeppli
Journal of medicinal chemistry
83
Citations
2
Influential Citations
Abstract
(-)-N-(Cyclopropylmethyl)-4,14-dimethoxymorphinan-6-one (2) was synthesized with 4,14-dimethoxy-N-methylmorphinan-6-one (1) as starting material. In vivo and in vitro experiments show 2 (cyprodime) to be a pure opioid receptor antagonist. Some of these tests (opioid receptor binding assays, guinea pig ileal longitudinal muscle preparation, rat and mouse vas deferens preparation, acetic acid writhing antagonism test) indicate that 2 is a selective mu opioid receptor antagonist.
Highly CitedCyprodime is a selective mu opioid receptor antagonist, showing potent opioid receptor antagonist activity in vivo and in vitro.
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