SRI-22136

SRI-22136 is a Delta opioid receptor (DOR) antagonist that can cross the blood-brain barrier with an IC50 of 0.42 nM. It lacks agonistic activity on DOR, MOR, and KOR, functioning solely as an antagonist with IC50 values of 370 nM for MOR and 54 nM for KOR, thereby avoiding addiction/aversion effects. SRI-22136 effectively inhibits DADLE (a DOR agonist) -induced BACE1 activity with an IC50 of 120 nM. It can completely prevent Alzheimer’s disease-like pathology in mouse models and is applicable for Alzheimer's research.