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ACS Chem Neurosci. 2014 Feb 19;5(2):93-9. doi: 10.1021/cn400205z. Epub 2014 Jan 8.

Preliminary pharmacological evaluation of enantiomeric morphinans.

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  • 1Alcohol & Drug Abuse Research Center, ‡Mailman Research Center, McLean Hospital, Harvard Medical School , 115 Mill Street, Belmont, Massachusetts 02478, United States.


A series of levo- and dextromorphinan pairs have been synthesized and evaluated for their affinities to the mu, kappa, and delta opioid receptors, the N-methyl-D-aspartate (NMDA) channel, and sigma 1 and 2 receptors. It was found that levo isomers tended to have higher affinities at the opioid receptors and moderate to high affinities to the NMDA and sigma receptors, while dextro isomers tended to have lower affinities to the opioid receptors but comparatively higher affinities to the NMDA and sigma receptors. This series of compounds have interesting and complex pharmacological profiles, and merit further investigation as potential therapies for drug abuse treatment.

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