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Description

A blood-brain-barrier-permeant, non-toxic, tertiary amide compound that acts as a high affinity, potent, multimodal blocker of RAGE (Receptor for Advanced Glycation End products) V domain-mediated ligand binding (Ki = 25, 148, and 230 nM, respectively, against A&beta,40, HMGB1, and S100B, binding to sRAGE). Blocks RAGE-mediated influx of A&beta,40 and A&beta,42 into the brain. Also shown to suppress A&beta,-RAGE induced NF-&kappa,B activation and NF-&kappa,B-dependent transcription of &beta,-secretase. Daily treatment of APPsw/0 murine AD model (1 mg/kg/d via i.p.) is reported to greatly reduce Thioflavin S-positive amyloid plaques in cortex and hippocampus (by 70 to 80%) and restore congnitive performance to the level of non-AD mice.