MF 268

MF 268 is an orally active, blood-brain barrier-permeable acetylcholinesterase (AChE) inhibitor with an IC₅₀ of 9 nM in rats. MF 268 binds to both the catalytic site and the regulatory anionic site of acetylcholinesterase, and increases the extracellular levels of acetylcholine, norepinephrine, dopamine and serotonin in the rat cortex via a dose-dependent pathway. MF 268 exhibits anti-amnesic effects in rats. MF 268 can be used in research related to Alzheimer's disease^[1][2]. In Vitro:MF 268 (120 min) potently inhibits acetylcholinesterase from rat whole brain in vitro, with an IC₅₀ of 9 nM^[2]. In Vivo:MF 268 (0.5-5.0 mg/kg; p.o.; single administration) dose-dependently increases extracellular acetylcholine (ACh), norepinephrine (NE) and dopamine (DA) in the cerebral cortex of healthy rats^[1].
MF 268 (0.5-2.0 mg/kg; s.c.; single dose) dose-dependently increases extracellular acetylcholine levels in the cortex of healthy rats, while moderately inhibiting cholinesterase^[1].
MF 268 (50 μM; intracortical perfusion via microdialysis probe; continuous administration; 6 hr) increased extracellular ACh levels in the cortical cells of healthy rats by 5900%, while also altering the levels of NE, DA and 5-HT^[1].
MF 268 (2-12 mg/kg; p.o.; single administration) exerts a persistent and selective reversal effect on Scopolamine (HY-N0296)-induced amnesia in rats, and the inhibition rate of whole-brain cholinesterase remains at 55% at 360 min after administration at 5 mg/kg^[2].