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Papers of the Week

Papers: 14 May 2022 - 20 May 2022

2022 May


36 Suppl 1

Structure Activity Relationship and Biological Evaluation of Small Molecule Antagonists for G-Protein Coupled Receptor Associated with Neuropathic Pain.


Opioids are commonly prescribed for the treatment of neuropathic pain; however, their high rates of physical dependency and addiction raise concern. Given their adverse side effects, there is a need for new therapeutics that target non-opioid receptors. GPR183 (Epstein-Barr induced gene 2, EBI2) is a G-protein coupled receptor (GPCR) that plays a role in the transduction of neuropathic pain. SAE-14 is a novel molecule that is able to antagonize, or inhibit GPR183; thus, preventing the transmission of pain. To gain a better understanding of which substituents improve the binding between SAE-14 and GPR-183, it is necessary to synthesize several analogs of the molecule. We have developed a structure-activity-relationship for GPR183 antagonism and the results from this gives a better understanding of the functional groups that are necessary for GPR183 antagonism and improve to the compound's potential therapeutic for neuropathic pain treatment.