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Zhang, Q. et al.

Discovery of novel triazole-based opioid receptor antagonists.

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).[1]

References

Discovery of novel triazole-based opioid receptor antagonists. Zhang, Q., Keenan, S.M., Peng, Y., Nair, A.C., Yu, S.J., Howells, R.D., Welsh, W.J. J. Med. Chem. (2006) [Pubmed]

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