Enkephalin analogues with a 4-anilidopiperidine scaffold have been designed and synthesized to achieve therapeutic benefit for the treatment of pain due to mixed μ and δ 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 μ and δ 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.
|Original language||English (US)|
|Number of pages||5|
|Journal||Journal of Medicinal Chemistry|
|State||Published - Nov 1 2007|
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery