Abstract：
:Ligands from the naltrexamine series have consistently demonstrated agonist activity at kappa opioid receptors (KOR), with varying activity at the mu opioid receptor (MOR). Various 6 beta-cinnamoylamino derivatives were made with the aim of generating ligands with a KOR agonist/MOR partial agonist profile, as ligands with this activity may be of interest as treatment agents for cocaine abuse. The ligands all displayed the desired high affinity, nonselective binding in vitro and in the functional assays were high efficacy KOR agonists with some partial agonist activity at MOR. Two of the new ligands (12a, 12b) have been evaluated in vivo, with 12a acting as a KOR agonist and therefore somewhat similar to the previously evaluated analogues 3-6, while 12b displayed predominant MOR agonist activity.
journal_name
J Med Chemjournal_title
Journal of medicinal chemistryauthors
Cami-Kobeci G,Neal AP,Bradbury FA,Purington LC,Aceto MD,Harris LS,Lewis JW,Traynor JR,Husbands SMdoi
10.1021/jm8015552subject
Has Abstractpub_date
2009-03-26 00:00:00pages
1546-52issue
6eissn
0022-2623issn
1520-4804journal_volume
52pub_type
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