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J Med Chem. 2007 Nov 1;50(22):5528-32. Epub 2007 Oct 10.

Development of novel enkephalin analogues that have enhanced opioid activities at both mu and delta opioid receptors.

Author information

1
Department of Chemistry, University of Arizona, Tucson, Arizona 85721, USA.

Abstract

Enkephalin analogues with a 4-anilidopiperidine scaffold have been designed and synthesized to achieve therapeutic benefit for the treatment of pain due to mixed mu and delta opioid agonist activities. Ligand 16, in which a Dmt-substituted enkephalin-like structure was linked to the N-phenyl-N-piperidin-4-yl propionamide moiety, showed very high binding affinities (0.4 nM) at mu and delta receptors with an increased hydrophobicity (aLogP = 2.96). This novel lead compound was found to have very potent agonist activities in MVD (1.8 nM) and GPI (8.5 nM) assays.

PMID:
17927164
PMCID:
PMC2678914
DOI:
10.1021/jm061465o
[Indexed for MEDLINE]
Free PMC Article

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