Journal: The journal of pain : official journal of the American Pain Society
Article Title: A Novel Mu-Delta Opioid Agonist Demonstrates Enhanced Efficacy with Reduced Tolerance and Dependence in Mouse Neuropathic Pain Models
doi: 10.1016/j.jpain.2019.05.017
Figure Lengend Snippet: SRI-22141 Displayed High Affinity, Potency, and Efficacy at the MOR and DOR. Affinity (K I ), potency (EC 50 ), and efficacy (E MAX ) values at the MOR, DOR, and KOR derived as reported in the Methods. The reported efficacy values were normalized to the stimulation caused by positive control compound (100%; SNC80 for DOR and DAMGO for MOR) and vehicle (0%). Data reported as the mean ± SEM from N = 3 independent experiments performed in duplicate. The positive control compounds (naloxone, U50,488, SNC80, DAMGO) returned expected values in each assay, validating the results.
Article Snippet: For the quantitative βarr2 recruitment assay using MOR- and DOR-U20S PathHunter cells from DiscoveRx, the manufacturer’s protocol was followed for all steps.
Techniques: Derivative Assay, Positive Control, Binding Assay, Activity Assay