Ladostigil - CAS 209394-27-4
Catalog number: 209349-27-4
Category: Inhibitor
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Ladostigil, also called as TV-3,326, is a novel neuroprotective agent developed to treat neurodegenerative disorders sunch as Alzheimer’s disease. Ladostigil is a dual acetylcholine-butyrylcholineesterase and brain selective monoamine oxidase (MAO)-A and -B inhibitor in vivo (with little or no MAO inhibitory effect in the liver and small intestine).
Solid powder
[(3R)-3-(prop-2-ynylamino)-2,3-dihydro-1H-inden-5-yl] N-ethyl-N-methylcarbamate; (N-propargyl-(3R) aminoindan-5-yl)-ethyl methyl carbamate; Ladostigil; TV 3326; TV3326; TV-3326
2 g/cm3
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1.Functional connectivity in prenatally stressed rats with and without maternal treatment with ladostigil, a brain-selective monoamine oxidase inhibitor.
Goelman G1, Ilinca R, Zohar I, Weinstock M. Eur J Neurosci. 2014 Sep;40(5):2734-43. doi: 10.1111/ejn.12621. Epub 2014 May 26.
Stress during pregnancy in humans is known to be a risk factor for neuropsychiatric disorders in the offspring. Prenatal stress in rats caused depressive-like behavior that was restored to that of controls by maternal treatment with ladostigil (8.5 mg/kg per day), a brain-selective monoamine oxidase (MAO) inhibitor that prevented increased anxiety-like behavior in stressed mothers. Ladostigil inhibited maternal striatal MAO-A and -B by 45-50% at the time the pups were weaned. Using resting state-functional connectivity magnetic resonance imaging on rat male offspring of control mothers, and mothers stressed during gestation with and without ladostigil treatment, we identified neuronal connections that differed between these groups. The percentage of significant connections within a predefined predominantly limbic network in control rats was 23.3 within the right and 22.0 within the left hemisphere. Prenatal stress disturbed hemispheric symmetry, resulting in 30.
2.Dose-dependent effects of ladostigil on microglial activation and cognition in aged rats.
Weinstock M1, Bejar C, Schorer-Apelbaum D, Panarsky R, Luques L, Shoham S. J Neuroimmune Pharmacol. 2013 Mar;8(1):345-55. doi: 10.1007/s11481-013-9433-0. Epub 2013 Jan 17.
The current study determined the effects of chronic treatment of aging rats with ladostigil, a cholinesterase (ChE) and monoamine oxidase (MAO) inhibitor, at doses of 1 and 8.5 mg/kg/day, on novel object recognition (NOR) and reference memory in the Morris water maze (MWM). A dose of (1 mg/kg/day) did not inhibit ChE or MAO but prevented the loss of NOR and reference memory in the MWM that occurs at 20.5 months of age. This anti-aging effect was associated with a reduction in the expression of CD11b, a marker of microglial activation, in the fornix and parietal cortex and restoration of microglial morphology to that in young adult rats. Ladostigil (8.5 mg/kg/day) inhibited brain ChE by ≈30 % and MAO A and B by 55-59 %, and had a similar, or greater effect than the low dose on microglia, but was less effective in preventing the decline in NOR. Ladostigil (8.5 mg/kg/day) may have caused too much cortical ChE inhibition and acetylcholine elevation at 16 months when NOR was intact.
3.Multi target neuroprotective and neurorestorative anti-Parkinson and anti-Alzheimer drugs ladostigil and m30 derived from rasagiline.
Youdim MB1. Exp Neurobiol. 2013 Mar;22(1):1-10. doi: 10.5607/en.2013.22.1.1. Epub 2013 Mar 31.
Present anti-PD and -AD drugs have limited symptomatic activity and devoid of neuroprotective and neurorestorative property that is needed for disease modifying action. The complex pathology of PD and AD led us to develop several multi-target neuroprotective and neurorestorative drugs with several CNS targets with the ability for possible disease modifying activity. Employing the pharmacophore of our anti-parkinson drug rasagiline (Azilect, N-propagrgyl-1-R-aminoindan), we have developed a series of novel multi-functional neuroprotective drugs (A) [TV-3326 (N-propargyl-3R-aminoindan-5yl)-ethyl methylcarbamate)], with both cholinesterase-butyrylesterase and brain selective monoamine-oxidase (MAO) A/B inhibitory activities and (B) the iron chelator-radical scavenging-brain selective monoamine oxidase (MAO) A/B inhibitor and M30 possessing the neuroprotective and neurorescuing propargyl moiety of rasagiline, as potential treatment of AD, DLB and PD with dementia.
4.Dose-limiting inhibition of acetylcholinesterase by ladostigil results from the rapid formation and fast hydrolysis of the drug-enzyme complex formed by its major metabolite, R-MCPAI.
Moradov D1, Finkin-Groner E1, Bejar C1, Sunita P1, Schorer-Apelbaum D1, Barasch D1, Nemirovski A1, Cohen M1, Weinstock M2. Biochem Pharmacol. 2015 Mar 15;94(2):164-72. doi: 10.1016/j.bcp.2015.01.017. Epub 2015 Feb 7.
Ladostigil is a pseudo reversible inhibitor of acetylcholinesterase (AChE) that differs from other carbamates in that the maximal enzyme inhibition obtainable does not exceed 50-55%. This could explain the low incidence of cholinergic adverse effects induced by ladostigil in rats and human subjects. The major metabolite, R-MCPAI is believed to be responsible for AChE inhibition by ladostigil in vivo. Therefore we determined whether the ceiling in AChE inhibition resulted from a limit in the metabolism of ladostigil to R-MCPAI by liver microsomal enzymes, or from the kinetics of enzyme inhibition by R-MCPAI. Ladostigil reduces TNF-α in lipopolysaccharide-activated microglia. In vivo, it may also reduce pro-inflammatory cytokines by inhibiting AChE and increasing the action of ACh on macrophages and splenic lymphocytes. We also assessed the contribution of AChE inhibition in the spleen of LPS-injected mice to the anti-inflammatory effect of ladostigil.
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CAS 209394-27-4 Ladostigil

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