Ladostigil (C09-1142-684)

Ladostigil (TV-3326) is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO) , with IC 50 s of 37.1 and 31.8 μM for MAO-B and AChE , respectively. Ladostigil exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's diseaseIn VitroLadostigil (1-10 µM) exerts neuroprotective activities, including a prevention of the fall of the mitochondrial membrane potential (ψ), attenuation of apoptotic cascades and an inhibition of ROS production induced by OS insults. Ladostigil (1-10 µM) has a significant neuroprotective activity, including inhibition of caspase-3 activation, induction of Bcl-2 and reduction of Bad and Bax gene and protein expression in human neuroblastoma SK-N-SH cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoLadostigil (17 mg/kg; p.o. daily for 6 weeks) abolishes their hyperanxiety and depressive-like behaviour in the elevated plus maze (EPM) and forced swim tests (FST) tests in adulthood from puberty to prenatally-stressed rats. Ladostigil (50 μmol/kg; single p.o.) restores the loss of episodic memory in the object recognition test in rats. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Pathogen-free (SPF) Sprague-Dawley ratsDosage: 17 mg/kg Administration: P.o. (added to the drinking water) daily for 6 weeks Result: Inhibited brain MAO-A and B by more than 60%. Reduced hyperanxiety of male and female prenatally stressed (PS) rats in the EPM and depressive-like behaviour in the FST.IC50& Target:MAO-B 37.1 μM (IC 50 ) AChE 31.8 μM (IC 50 ). Molecular Formula: C16H20N2O2 Molecular Weight: 272.34 PubChem CID: 208907 Isomeric SMILES: CCN(C)C(=O)OC1=CC2=C(CC[C@H]2NCC#C)C=C1