Tacrine (hydrochloride)

Tacrine hydrochloride is a potent brain-penetrant inhibitor of both AChE and BChE, with IC₅₀s of 31 nM and 25.6 nM, respectively. Tacrine hydrochloride is also a NMDAR inhibitor, with an IC₅₀ of 26 μM. Tacrine hydrochloride can be used for the research of Alzheimer’s disease^[1][2]. IC50 & Target:IC50: 31 nM (AChE), 25.6 nM (BChE), 26 μM (NMDAR)^[1][2] In Vitro:Tacrine (12.5-37.5 nM) inhibits venom acetylcholinesterase as well as human serum butyrylcholinesterase in a concentration-dependent manner^[1].
Tacrine reduces the neurotoxicity induced by the activation of the NMDARs in murine cortical neuronal cultures with an IC₅₀of ~500 μM^[2].
Tacrine inhibits the NMDAR responses in a concentration-dependent manner with an IC₅₀ of ~190 μM at -60 mV^[2]. In Vivo:Tacrine (20-40 μmol/kg; s.c.) disrupts retention of learning in 17- and 30-day old mice in passive avoidance, and while the low dose of tacrine treatment (5 μmol/kg; s.c.) improves retention in 17-day old mice^[2].
Tacrine (0.1-0.4 mg/mL; i.p. for 7 d) inhibits the expression of AChE, but does not significantly improve the protection of the retina function and morphology in mice^[3].