Ladostigil
Names
[ CAS No. ]:
209394-27-4
[ Name ]:
Ladostigil
Biological Activity
[Description]:
Ladostigil (TV-3326) is a dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with an IC50 of 37.1 and 31.8 μM for MAO-B and AChE, reapectively. Ladostigil could increase cholinergic transmission, prevent the formation of ROS or their actions and be used for the research of depression and Alzheimer's disease[1][2].
[Related Catalog]:
[Target]
MAO-B:37.1 μM (IC50)
AChE:31.8 μM (IC50)
[In Vitro]
Ladostigil (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[2]. 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[2].
[In Vivo]
Ladostigil (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[4]. Ladostigil (50 μmol/kg; single p.o.) restores the loss of episodic memory in the object recognition test in rats[3]. Animal Model: Pathogen-free (SPF) Sprague-Dawley rats[4] Dosage: 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.
[References]
Chemical & Physical Properties
[ Molecular Formula ]:
C16H20N2O2
[ Molecular Weight ]:
272.34200
[ Exact Mass ]:
272.15200
[ PSA ]:
41.57000
[ LogP ]:
2.73810
[ Vapour Pressure ]:
5.19E-07mmHg at 25°C
Safety Information
[ Hazard Codes ]:
Xi