Identification of brain-permeant small molecule modulators of GAL1R receptor

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The mu opioid receptor is the major target of most potent analgesics (e.g. morphine). However, severe side effects such as dependence and respiratory depression have been associated with this receptor. Members of this project team have reported that a significant population of mu-opioid receptors (MOR) localized in the ventral tegmental area (VTA) form heteromers with galanin Gal1 receptors (GAL1R) which modulate dopamine cell function. As such, these MOR-GAL1R heteromers may represent a potential target for the treatment of opioid use disorder. The project team intends to screen in-house libraries to identify small molecules modulating GAL1R receptor. The hits will be profiled for selectivity, and medicinal chemistry will be undertaken for select molecules to further improve their efficacy and potency.