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Collybolide Is A Novel Biased Agonist Of Κ-Opioid Receptors With Potent Antipruritic Activity, Achla Gupta, Ivone Gomes, Erin N. Bobeck, Amanda K. Fakira, Nicholas P. Massaro, Indrajeet Sharma, Adrien Cavé, Heidi E. Hamm, Joseph Parello, Lakshmi A. Devi

Biology Faculty Publications

Among the opioid receptors, the κ-opioid receptor (κOR) has been gaining considerable attention as a potential therapeutic target for the treatment of complex CNS disorders including depression, visceral pain, and cocaine addiction. With an interest in discovering novel ligands targeting κOR, we searched natural products for unusual scaffolds and identified collybolide (Colly), a nonnitrogenous sesquiterpene from the mushroom Collybia maculata. This compound has a furyl-δ-lactone core similar to that of Salvinorin A (Sal A), another natural product from the plant Salvia divinorum. Characterization of the molecular pharmacological properties reveals that Colly, like Sal A, is a highly potent and selective …