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Science 22 April 1983:
Vol. 220. no. 4595, pp. 417 - 418
DOI: 10.1126/science.6301007
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Articles

Science, Vol 220, Issue 4595, 417-418
Copyright © 1983 by American Association for the Advancement of Science

articles

Methadone conformation and opioid activity

WL Duax, GD Smith, JF Griffin, and PS Portoghese

The inactive methadone analog threo-5-methylmethadone has a solid-state conformation in which the nitrogen is antiperiplanar to the tertiary carbon C(4). Since threo-5-methylmethadone exhibits no opioid agonism either in vivo or in vitro, methadone analogs probably do not have this conformation when bound to an opioid receptor. The potent agonist (-)-erythro-5-methylmethadone has a solid-state conformation in which the nitrogen atom is rotated back toward the phenyl rings on the quarternary carbon, suggesting that this unusual conformation is the active one.




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Science. ISSN 0036-8075 (print), 1095-9203 (online)