H3R antagonist 4

Description

H3R antagonist 4 compound 11L was a dual inhibitor of cholinesterase and histamine receptor H3R , with corresponding IC50 of 7.04 ?M eeAChE , 9.73 ?M hAChE reversible and 1.09 nM H3R , respectively. H3R antagonist 4 inhibited the aggregation of A?1-42 induced by itself and Cu2+ 95.48 % and 88.63 % , and degraded the A?1-42 fibrils induced by itself and Cu2+ 80.16 % and 89.30 % . H3R antagonist 4 chelate biometals such as Cu2+, Zn2+, Al3+, and Fe2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by A?1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimers disease induced by scopolamine HY-N0296 .