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  • Title: 2,4-Diaminopyridine delta-opioid receptor agonists and their associated hERG pharmacology.
    Author: Owen DR, Rodriguez-Lens M, Corless MD, Gaulier SM, Horne VA, Kinloch RA, Maw GN, Pearce DW, Rees H, Ringer TJ, Ryckmans T, Stammen BL.
    Journal: Bioorg Med Chem Lett; 2009 Mar 15; 19(6):1702-6. PubMed ID: 19231185.
    Abstract:
    A number of libraries were produced to explore the potential of 2,4-diaminopyridine lead 1. The resulting diaminopyridines proved to be potent and selective delta-opioid receptor agonists. Several rounds of lead optimisation using library chemistry identified compound 17 which went on to show efficacy in an electromyography model of neuropathic pain. The structure-activity relationship of the series against the hERG ion channel proved to be a key selectivity hurdle for the series.
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