P11149, a derivative of Galanthamine, acts as a competitive, orally active, and selective AChE inhibitor with the ability to weakly penetrate the blood-brain barrier (BBB). It demonstrates selective inhibition, exhibiting an IC50 of 1.3 μM for rat BChE/AChE, and shows central cholinergic activity, behavioral efficacy, and safety. P11149 is utilized in Alzheimer’s disease research[1].

BChE/AChE (rat):1.3 μM (IC50)

P11149 is a GAL analog that, upon rapid in vivo hydrolyzation, produces 6-DMG, a potent AChE inhibitor. It demonstrates superior subcutaneous (s.c.) bioavailability compared to oral (p.o.) administration. In mice, oral doses of P11149 induce salivation (Sal), lacrimation (Lac), and tremors at levels comparable to those observed in rats. Notably, 6-DMG, P1 1012, and GAL trigger Sal and Lac at lower doses in rats. Moreover, P11149 has a half-life (T1/2(el)) of 2.4 hours and reaches a maximum concentration (Cmax) of 585 ng/mL in rat plasma.