Details
Stereochemistry | ABSOLUTE |
Molecular Formula | 2C16H20N2O2.C4H6O6 |
Molecular Weight | 694.7712 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 4 / 4 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O[C@H]([C@@H](O)C(O)=O)C(O)=O.CCN(C)C(=O)OC1=CC2=C(CC[C@H]2NCC#C)C=C1.CCN(C)C(=O)OC3=CC4=C(CC[C@H]4NCC#C)C=C3
InChI
InChIKey=PRLVBVAJMQZMJN-OGOSNNLPSA-N
InChI=1S/2C16H20N2O2.C4H6O6/c2*1-4-10-17-15-9-7-12-6-8-13(11-14(12)15)20-16(19)18(3)5-2;5-1(3(7)8)2(6)4(9)10/h2*1,6,8,11,15,17H,5,7,9-10H2,2-3H3;1-2,5-6H,(H,7,8)(H,9,10)/t2*15-;1-,2-/m111/s1
Molecular Formula | C16H20N2O2 |
Molecular Weight | 272.3422 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
Molecular Formula | C4H6O6 |
Molecular Weight | 150.0868 |
Charge | 0 |
Count |
|
Stereochemistry | ABSOLUTE |
Additional Stereochemistry | No |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Optical Activity | UNSPECIFIED |
LADOSTIGIL, a rasagiline derivative, is a reversible acetylcholinesterase and butyrylcholinesterase inhibitor with neuroprotective properties. It also acts as an irreversible brain monoamine oxidases inhibitor. It is under development for the treatment of neurodegenerative disorders like dementia and Alzheimer's disease.
CNS Activity
Originator
Approval Year
PubMed
Title | Date | PubMed |
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Protein 4.1N is required for translocation of inositol 1,4,5-trisphosphate receptor type 1 to the basolateral membrane domain in polarized Madin-Darby canine kidney cells. | 2003 Feb 7 |
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Inactivation of purified human recombinant monoamine oxidases A and B by rasagiline and its analogues. | 2004 Mar 25 |
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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. | 2005 Aug |
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Bifunctional drug derivatives of MAO-B inhibitor rasagiline and iron chelator VK-28 as a more effective approach to treatment of brain ageing and ageing neurodegenerative diseases. | 2005 Feb |
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Rasagiline: neurodegeneration, neuroprotection, and mitochondrial permeability transition. | 2005 Jan 1-15 |
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The neurochemical and behavioral effects of the novel cholinesterase-monoamine oxidase inhibitor, ladostigil, in response to L-dopa and L-tryptophan, in rats. | 2005 Oct |
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Ladostigil, a novel multifunctional drug for the treatment of dementia co-morbid with depression. | 2006 |
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Implications of co-morbidity for etiology and treatment of neurodegenerative diseases with multifunctional neuroprotective-neurorescue drugs; ladostigil. | 2006 Dec |
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The path from anti Parkinson drug selegiline and rasagiline to multifunctional neuroprotective anti Alzheimer drugs ladostigil and m30. | 2006 Dec |
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A multifunctional, neuroprotective drug, ladostigil (TV3326), regulates holo-APP translation and processing. | 2006 Oct |
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Chronic brain cytochrome oxidase inhibition selectively alters hippocampal cholinergic innervation and impairs memory: prevention by ladostigil. | 2007 Aug |
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Induction of neurotrophic factors GDNF and BDNF associated with the mechanism of neurorescue action of rasagiline and ladostigil: new insights and implications for therapy. | 2007 Dec |
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The application of proteomics and genomics to the study of age-related neurodegeneration and neuroprotection. | 2007 Feb |
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Ladostigil prevents gliosis, oxidative-nitrative stress and memory deficits induced by intracerebroventricular injection of streptozotocin in rats. | 2007 Mar |
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Aminoindan and hydroxyaminoindan, metabolites of rasagiline and ladostigil, respectively, exert neuroprotective properties in vitro. | 2007 Oct |
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The effects of rivastigmine plus selegiline on brain acetylcholinesterase, (Na, K)-, Mg-ATPase activities, antioxidant status, and learning performance of aged rats. | 2008 Aug |
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The neuroprotective mechanism of action of the multimodal drug ladostigil. | 2008 May 1 |
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The neuroprotective effect of ladostigil against hydrogen peroxide-mediated cytotoxicity. | 2008 Sep 25 |
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The neurotrophic and neuroprotective effects of psychotropic agents. | 2009 |
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Activation of mGlu3 receptors stimulates the production of GDNF in striatal neurons. | 2009 Aug 12 |
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Interaction between environmental and genetic factors modulates schizophrenic endophenotypes in the Snap-25 mouse mutant blind-drunk. | 2009 Dec 1 |
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The novel cholinesterase-monoamine oxidase inhibitor and antioxidant, ladostigil, confers neuroprotection in neuroblastoma cells and aged rats. | 2009 Feb |
|
Why do we need multifunctional neuroprotective and neurorestorative drugs for Parkinson's and Alzheimer's diseases as disease modifying agents. | 2010 Jun |
Substance Class |
Chemical
Created
by
admin
on
Edited
Wed Jul 05 23:10:59 UTC 2023
by
admin
on
Wed Jul 05 23:10:59 UTC 2023
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Record UNII |
2J1346C51H
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Record Status |
Validated (UNII)
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Record Version |
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-
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NCI_THESAURUS |
C47792
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NCI_THESAURUS |
C667
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300000044446
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CHEMBL255231
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209394-46-7
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C76072
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QQ-52
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2J1346C51H
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11607225
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DTXSID60175107
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PARENT -> SALT/SOLVATE | |||
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ACTIVE MOIETY |