Discovery of novel triazole-based opioid receptor antagonists.

ID: ALA1138930

Journal: J Med Chem

Title: Discovery of novel triazole-based opioid receptor antagonists.

Authors: Zhang Q, Keenan SM, Peng Y, Nair AC, Yu SJ, Howells RD, Welsh WJ.

Abstract: We report the computer-aided design, chemical synthesis, and biological evaluation of a novel family of delta opioid receptor (DOR) antagonists containing a 1,2,4-triazole core structure that are structurally distinct from other known opioid receptor active ligands. Among those delta antagonists sharing this core structure, 8 exhibited strong binding affinity (K(i) = 50 nM) for the DOR and appreciable selectivity for delta over mu and kappa opioid receptors (delta/mu = 80; delta/kappa > 200).

CiteXplore: 16821764

DOI: 10.1021/jm0601250

Patent ID: ┄