| Identification | Back Directory | [Name]
Carbamic acid, ethylmethyl-, (3R)-2,3-dihydro-3-(2-propynylamino)-1H-inden-5-yl ester, monohydrochloride (9CI) | [CAS]
209394-18-3 | [Synonyms]
Ladostigil hydrochloride
Carbamic acid, ethylmethyl-, (3R)-2,3-dihydro-3-(2-propynylamino)-1H-inden-5-yl ester, monohydrochloride (9CI) | [Molecular Formula]
C16H21ClN2O2 | [MOL File]
209394-18-3.mol | [Molecular Weight]
308.81 |
| Hazard Information | Back Directory | [Uses]
Ladostigil (TV-3326) hydrochloride is an orally active dual inhibitor of cholinesterase and brain-selective monoamine oxidase (MAO), with IC50s of 37.1 and 31.8 μM for MAO-B and AChE, respectively. Ladostigil hydrochloride exhibits neuroprotective, antioxidant and anti-inflammatory activities. Ladostigil can be used for the research of depression and Alzheimer's disease[1][2]. Ladostigil (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [in vivo]
Ladostigil (17 mg/kg; p.o. daily for 6 weeks) hydrochloride 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.) hydrochloride 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: | Oral (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.
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| [IC 50]
AChE: 31.8 μM (IC50); MAO-B: 37.1 μM (IC50) | [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. DOI:10.1039/c7md00569e
[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. DOI:10.2174/138945012799499794
[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. DOI:10.1007/978-3-211-45295-0_67
[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. DOI:10.1007/s00213-005-2229-z |
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