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  • Title: Probing opioid receptor interactions with azacycloalkane amino acids. Synthesis of a potent and selective ORL1 antagonist.
    Author: Halab L, Becker JA, Darula Z, Tourwé D, Kieffer BL, Simonin F, Lubell WD.
    Journal: J Med Chem; 2002 Nov 21; 45(24):5353-7. PubMed ID: 12431062.
    Abstract:
    Azacycloalkane turn mimics 6-9 were used to explore the relationship between conformation and biological activity of peptide ligands to the opioid receptor-like (ORL1) receptor. Three azabicyclo[x.y.0]alkane amino acids and a 5-tBuPro type VI beta-turn mimic were introduced into peptides 10-13 by solid-phase synthesis on MBHA resin. Biological examination of peptides 10-13 showed two new antagonists (10 and 12) exhibiting increased selectivity for the ORL1 receptor.
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