Salvinorin A is a neo-clerodane diterpenoid. It is not soluble in water or lipids, which is a significant hurdle for clinical deliverable formulation. In contrast to classic KOR ligands, salvinorin A is not an alkaloid, indicating that it cannot be rendered into a salt to improve solubility for drug development purposes. The melting point of salvinorin A is high (238-240 °C) [5], and the powder form of salvinorin A is relatively stable. However, once taken, salvinorin A is hydrolyzed quickly by esterases due to the hydrolyzable nature of the ester functional group at C2, which is an advantage for clinical practices that need the benefits of a KOR agonist with a shortacting property and a short duration of hallucinatory or dissociative side effects. Molecular Target of Salvinorin ASalvinorin A (Figure 1) was first isolated from Salvia divinorum in 1982 by Ortega and coworkers [6], and it is one of the most potent, naturally occurring opioid agonists, with high selectivity and affinity towards KORIn 2002, Roth and coworkers discovered that salvinorin A targeted KORs expressed in both human embryonic kidney-293 cells (K i = 16 nM) and guinea pig brain (K i = 4.3 nM) [1]. They also discovered the nonbiased agonism nature of salvinorin A towards KOR when it was observed to activate both the G-protein signaling pathway (EC 50 in cAMP assay = 4.73 nM) and β-arrestin-recruitment pathway (EC 50 in the Tango assay = 10.5 nM) [8].
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