Open AccessPreliminary Pharmacological Evaluation of Enantiomeric Morphinans
Author(s) -
Anna W. Sromek,
Brian A. Provencher,
Shayla Russell,
Elena H. Chartoff,
Brian I. Knapp,
Jean M. Bidlack,
John L. Neumeyer
Publication year - 2014
Publication title -
acs chemical neuroscience
Language(s) - Uncategorized
Resource type - Journals
SCImago Journal Rank - 1.158
H-Index - 69
ISSN - 1948-7193
DOI - 10.1021/cn400205z
Subject(s) - affinities , receptor , opioid , nmda receptor , chemistry , enantiomer , sigma receptor , pharmacology , stereochemistry , biology , biochemistry
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.