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  • Title: Discovery of N-(2-hydroxy-2-aryl-cyclohexyl) substituted spiropiperidines as GlyT1 antagonists with improved pharmacological profile.
    Author: Ceccarelli SM, Pinard E, Stalder H, Alberati D.
    Journal: Bioorg Med Chem Lett; 2006 Jan 15; 16(2):354-7. PubMed ID: 16246561.
    Abstract:
    During SAR exploration of N-(2-aryl-cyclohexyl) substituted spiropiperidine as GlyT1 inhibitors, it was found that introduction of an hydroxy group in position 2 of the cyclohexyl residue considerably improves the pharmacological profile. In particular, reduction of the binding affinity at the nociceptin/orphanin FQ peptide and the mu opioid receptors was achieved.
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