Abstract
An SAR study on the Dmt-substituted enkephalin-like tetrapeptide with a N-phenyl-N-piperidin-4-ylpropionamide moiety at the C-terminal was performed and has resulted in highly potent ligands at μ and δ opioid receptors. In general, ligands with the substitution of d-Nle2 and halogenation of the aromatic ring of Phe4 showed highly increased opioid activities. Ligand 6 with good biological activities in vitro demonstrated potent in vivo antihyperalgesic and antiallodynic effects in the tail-flick assay.
Original language | English (US) |
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Pages (from-to) | 382-386 |
Number of pages | 5 |
Journal | Journal of Medicinal Chemistry |
Volume | 54 |
Issue number | 1 |
DOIs | |
State | Published - Jan 13 2011 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery