SRI-22136

SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC50 of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC50 = 370 nM), KOR (IC50 = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (IC50 = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease[1].

C30H29ClN2O3

501.02

ClC(C=C1)=CC=C1C2=CC(C[C@]([C@H](N(CC3)CC4CC4)C5)(OC)[C@@]63C7=C5C=CC(O)=C7O[C@@H]86)=C8N=C2

Beta-secretase; Opioid Receptor

BACE1; δ Opioid Receptor/DOR; κ Opioid Receptor/KOR; μ Opioid Receptor/MOR

Room temperature