1. AChE (Acetylcholinesterase) inhibitor
TAK-147
AChE (Acetylcholinesterase) inhibitor
Summary
TAK-147, a potent acetylcholinesterase (AChE) inhibitor, potentiated choline acetyltransferase (ChAT) activity in cultured rat septal cholinergic neurons in a concentration-dependent manner with an EC50 value of 4.47 nM.
Safety, tolerability and adverse events
Pre-clinical pharmacology
TAK-147 potently inhibited the AChE activity of rat cerebral cortex extract with an IC50 value of 51.2 nM.
TAK-147 at the dose of 10 mg/kg reduced AChE activity in the cerebral cortex by 52.7% 1 hr after its administration. Even at 1 mg/kg TAK-147 caused a slight but significant inhibition of AChE activity (89.1% of control).
Clinical studies
Exclusion/restrictions to future studies
Other relevant information