Synonyms: AE-37 | AE37 | Anavex 2-73 | Anavex2-73 | THD-DP-FM
Compound class:
Synthetic organic
Comment: Blarcamesine (Anavex2-73) is a Sigma-1 (σ1) protein agonist and muscarinic acetylcholine receptor modulator [6]. Anavex are investigating it for potential to slow progression in neurodegenerative conditions including Parkinson's and Alzheimer's diseases, and Rett syndrome [2]. Anticonvulsant, anti-amnesic, neuroprotective and antidepressant activities in response to blarcamesine have been identified in a number of animal models of neurodegenerative and neurodevelopmental conditions [3-6].
Ligand Activity Visualisation ChartsThese are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts. ✖ |
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References |
1. Hampel H, Williams C, Etcheto A, Goodsaid F, Parmentier F, Sallantin J, Kaufmann WE, Missling CU, Afshar M. (2020)
A precision medicine framework using artificial intelligence for the identification and confirmation of genomic biomarkers of response to an Alzheimer's disease therapy: Analysis of the blarcamesine (ANAVEX2-73) Phase 2a clinical study. Alzheimers Dement (N Y), 6 (1): e12013. [PMID:32318621] |
2. Kaufmann WE, Sprouse J, Rebowe N, Hanania T, Klamer D, Missling CU. (2019)
ANAVEX®2-73 (blarcamesine), a Sigma-1 receptor agonist, ameliorates neurologic impairments in a mouse model of Rett syndrome. Pharmacol Biochem Behav, 187: 172796. [PMID:31704481] |
3. Lahmy V, Long R, Morin D, Villard V, Maurice T. (2014)
Mitochondrial protection by the mixed muscarinic/σ1 ligand ANAVEX2-73, a tetrahydrofuran derivative, in Aβ25-35 peptide-injected mice, a nontransgenic Alzheimer's disease model. Front Cell Neurosci, 8: 463. [PMID:25653589] |
4. Lahmy V, Meunier J, Malmström S, Naert G, Givalois L, Kim SH, Villard V, Vamvakides A, Maurice T. (2013)
Blockade of Tau hyperphosphorylation and Aβ₁₋₄₂ generation by the aminotetrahydrofuran derivative ANAVEX2-73, a mixed muscarinic and σ₁ receptor agonist, in a nontransgenic mouse model of Alzheimer's disease. Neuropsychopharmacology, 38 (9): 1706-23. [PMID:23493042] |
5. Maurice T. (2016)
Protection by sigma-1 receptor agonists is synergic with donepezil, but not with memantine, in a mouse model of amyloid-induced memory impairments. Behav Brain Res, 296: 270-278. [PMID:26386305] |
6. Villard V, Espallergues J, Keller E, Vamvakides A, Maurice T. (2011)
Anti-amnesic and neuroprotective potentials of the mixed muscarinic receptor/sigma 1 (σ1) ligand ANAVEX2-73, a novel aminotetrahydrofuran derivative. J Psychopharmacol, 25 (8): 1101-17. [PMID:20829307] |