Ladostigil hemitartrate (TV-3326) is a dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50 values of 37.1 μM for MAO-B and 31.8 μM for AChE. Possessing neuroprotective, antioxidant, and anti-inflammatory properties, it is commonly used in research related to depression and Alzheimer's disease.

AChE:31.8 nM (IC50), MAO-B:37.1 nM (IC50)

Ladostigil hemitartrate (1-10 μM) demonstrates significant neuroprotective properties by preventing the decrease of mitochondrial membrane potential (ψ), attenuating apoptotic cascades, and inhibiting ROS production triggered by oxidative stress (OS) insults[2]. Additionally, it inhibits caspase-3 activation, upregulates Bcl-2, and decreases Bad and Bax gene and protein expression in human neuroblastoma SK-N-SH cells[2].

Ladostigil hemitartrate, administered orally at 17 mg/kg daily for six weeks, effectively eliminates hyperanxiety and depressive-like behaviors in Sprague-Dawley rats, observed through the elevated plus maze (EPM) and forced swim tests (FST) from puberty into adulthood. This treatment regimen notably inhibited brain monoamine oxidase A and B (MAO-A and B) activity by over 60% and mitigated the heightened anxiety and depressive symptoms in both male and female rats prenatally stressed (PS). Additionally, a single oral dose of Ladostigil hemitartrate at 50 μmol/kg was sufficient to reverse episodic memory loss in the object recognition test in rats, showcasing its potential therapeutic effects on memory impairments.