Abstract
Partially modified retro-inverso, retro, and inverso isomers of hydrazide linked bifunctional peptides were designed, synthesized, and evaluated for bioactivities at δ/μ opioid receptors and CCK-1/CCK-2 receptors. All modifications of the CCK pharmacophore moiety affected bioactivities for the CCK-1 and CCK-2 receptors (up to 180-fold increase in the binding affinity with higher selectivity) and for the δ and μ opioid receptors. The results indicate that the opioid and CCK pharmacophores in one molecule interact with each other to induce topographical changes for both pharmacophores.
Original language | English (US) |
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Pages (from-to) | 165-168 |
Number of pages | 4 |
Journal | Journal of Medicinal Chemistry |
Volume | 50 |
Issue number | 1 |
DOIs | |
State | Published - Jan 1 2007 |
ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery