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, 45 (24), 5353-7

Probing Opioid Receptor Interactions With Azacycloalkane Amino Acids. Synthesis of a Potent and Selective ORL1 Antagonist

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Probing Opioid Receptor Interactions With Azacycloalkane Amino Acids. Synthesis of a Potent and Selective ORL1 Antagonist

Liliane Halab et al. J Med Chem.

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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