Abstract
A series of naltrexone-derived pyridomorphinans possessing various substituents at the 5′-position on the pyridine ring were synthesized and evaluated for opioid receptor binding in rodent brain membranes and functional activity in smooth muscle preparations. While the introduction of aromatic 1-pyrrolyl group (6h) improved the δ affinity and δ antagonist potency of the parent compound (3), the introduction of guanidine group (6i) transformed it to a κ selective ligand in opioid receptor binding and [35S]GTP-γ-S functional assays.
Original language | English (US) |
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Pages (from-to) | 529-532 |
Number of pages | 4 |
Journal | Bioorganic and Medicinal Chemistry Letters |
Volume | 13 |
Issue number | 3 |
DOIs | |
State | Published - Feb 2003 |
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Molecular Biology
- Pharmaceutical Science
- Drug Discovery
- Clinical Biochemistry
- Organic Chemistry