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Synonyms: EHT-0202 | SQ 20009
Compound class: Synthetic organic
Comment: Has anxiolytic effects as positive allosteric modulator of the GABAA receptor at the barbiturate binding site, as an adenosine antagonist of the A1 and A2 receptor subtypes and as a phosphodiesterase inhibitor selective for the PDE4 isoform. It is currently in clinical trials for the treatment of Alzheimer's disease with a possible MMOA of upregulating alpha-secretase activity.
Ligand Activity Visualisation Charts
These 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.✖
1. Marcade M, Bourdin J, Loiseau N, Peillon H, Rayer A, Drouin D, Schweighoffer F, Désiré L. (2008)
Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing.
J. Neurochem., 106 (1): 392-404. [PMID:18397369]
2. Vellas B, Sol O, Snyder PJ, Ousset PJ, Haddad R, Maurin M, Lemarié JC, Désiré L, Pando MP, EHT0202/002 study group. (2011)
EHT0202 in Alzheimer's disease: a 3-month, randomized, placebo-controlled, double-blind study.
Curr Alzheimer Res, 8 (2): 203-12. [PMID:21222604]
3. Zezula J, Slany A, Sieghart W. (1996)
Interaction of allosteric ligands with GABAA receptors containing one, two, or three different subunits.
Eur. J. Pharmacol., 301 (1-3): 207-14. [PMID:8773466]