Rivastigmine 是具有口服活性的、有效的、可透过血脑屏障的胆碱酯酶抑制剂，可抑制丁酰胆碱酯酶和乙酰胆碱酯酶，IC50分别为 0.037 μM 和 4.15 μM。它是一种拟副交感神经剂或胆碱能剂，用于研究轻度至中度阿尔茨海默氏型痴呆和帕金森氏病引起的痴呆。

Rivastigmine is a Cholinesterase Inhibitor, used for therapy of Alzheimer disease.

Preclinical biochemical studies indicates that rivastigmine has central nervous system selectivity over peripheral inhibition. It ameliorates memory impairment in rats with forebrain lesions. The drug is rapidly absorbed orally, with a bioavailability of 0.355 and low protein binding (40%). Its elimination halflife is less than 2 hours, and it is converted to an inactive metabolite at the site of action, bypassing hepatic metabolic pathways. Its disposition essentially is unaltered in patients with renal or hepatic impairment. It also has dosedependent effects on AChE inhibition[1].

Chronic toxicity is assessed 7 days after continuous exposure of cells to donepezil or rivastigmine using cell viability and cell esterase activity and the estimated cell numbers as parameters for viability. Culture medium including the tested drugs is changed once after 4 days.(Only for Reference)

123441-03-2

C14H22N2O2

250.342

利凡斯的明;S-Rivastigmine;SDZ-ENA 713;卡巴拉汀;Exelon

DMSO:50 mg/mL (199.73 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years