Naphtho and benzo analogs of the .kappa. opioid agonist trans-(.+-.)-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzeneacetamide
- 1 June 1991
- journal article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 34 (6) , 1891-1896
- https://doi.org/10.1021/jm00110a021
Abstract
Further elaboration on the structure-activity relationships in our U-50,488 series has revealed that benzologation of this cyclohexane-1,2-diamine derivative provides compounds which either maintain the interaction with the kappa receptor (e.g. compounds 3a and 5a in the phenylacetamido series) or eliminate the mu receptor mediated analgesia (e.g. compounds 3-6 in the benzamido series). Naphthologation also caused the elimination of mu receptor mediated analgesia (e.g. compounds 17a and 17b).Keywords
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