209394-27-4

209394-27-4 structure

Name: Ladostigil
Chemical Name: Ladostigil
CAS Number: 209394-27-4
Molecular Formula: C₁₆H₂₀N₂O₂
Molecular Weight: 272.34200
Catalog: Signaling Pathways Neuronal Signaling AChE
Create Date: 2016-08-04 03:24:06
Modify Date: 2024-01-02 16:02:43
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].

Name	Ladostigil

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	Signaling Pathways >> Neuronal Signaling >> Monoamine Oxidase Research Areas >> Neurological Disease Signaling Pathways >> Neuronal Signaling >> AChE
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	[1]. Denya I, et, al. Design, synthesis and evaluation of indole derivatives as multifunctional agents against Alzheimer's disease. Medchemcomm. 2018 Jan 16; 9(2):357-370. [2]. Weinreb O, et, al. Ladostigil: a novel multimodal neuroprotective drug with cholinesterase and brain-selective monoamine oxidase inhibitory activities for Alzheimer's disease treatment. Curr Drug Targets. 2012 Apr; 13(4): 483-94. [3]. Weinstock M, et, al. Ladostigil, a novel multifunctional drug for the treatment of dementia co-morbid with depression. J Neural Transm Suppl. 2006; (70):443-6. [4]. Poltyrev T, et, al. Effect of chronic treatment with ladostigil (TV-3326) on anxiogenic and depressive-like behaviour and on activity of the hypothalamic-pituitary-adrenal axis in male and female prenatally stressed rats. Psychopharmacology (Berl). 2005 Aug;181(1): 118-25.

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

Hazard Codes	Xi

Precursor 0
DownStream 1
209394-46-7

209394-27-4	209394-46-7
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849349-65-1