产品描述:
Rivastigmine is a cholinesterase (ChE) inhibitor that inhibits butyryl ChE (BChE) and acetyl ChE (AChE; IC50s = 0.037 and 4.15 μM, respectively).{24084} It increases levels of secreted amyloid precursor protein (sAPP) and decreases levels of soluble amyloid-β (1-40) and various N-terminal cleavage products in primary embryonic rat neurons undergoing degeneration when used at concentrations of 5 and 10 μM.{36871}. In a rat model of Alzheimer's disease induced by aluminum chloride (AlCl3), rivastigmine (1 mg/kg per day) inhibits formation of amyloid plaques in brain sections and increases in AChE, IL-1β, and β-secretase 1 (BACE1) mRNA expression in the cerebral cortex.{36872} It inhibits AlCl3-induced increases in escape latency time in the Morris water maze in a rat model of Alzheimer's disease when administered at a dose of 1 mg/kg. Rivastigmine (2 mg/kg) also reverses decreases in time spent in the open arms of an elevated plus maze, exploration time of a novel object in a novel object recognition test, and sucrose intake in a rat model of chronic mild stress.{36873} Formulations containing rivastigmine have been used in the treatment of dementia associated with Alzheimer's disease and Parkinson's disease.