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 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) |
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Pages (from-to) | 5528-5532 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 50 |
Issue number | 22 |
DOIs | |
State | Published - Nov 1 2007 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery