A cell-permeable, blood-brain barrier permeant, non-toxic phenethylpiperidine compound that binds reversibly and with high affinity to the uOR-deltaOR-heteromer. Exhibits a robust beta-arrestin recruitment activity (EC50 = 8.3uM; Emax = 1,197% over basal), which is at least two to three-fold higher than that obtained with ubetagalOR (EC50 = 1.8uM; Emax = 557%) or deltabetagalOR (EC50 = 2.7uM; Emax = 423%) alone. Induces a strong increase in [35S]GTPupsilonS binding (EC50 = 54, 210, and 300nM; and Emax (% basal) = 168, 138 and 113 for with ubetagalOR-deltaOR, ubetagalOR and deltabetagalOR, respectively). Potentiates antinociceptive activity similar to morphine (10mg/kg, s.c. in a tail-flick assay) with less side effects and dependency. However, chronic administration of CYM51010 results in reduced antinociceptive tolerance compared with morphine.
Storage and Stability:May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer.
