Details
Stereochemistry | ACHIRAL |
Molecular Formula | C14H19N5O2.ClH |
Molecular Weight | 325.794 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Cl.CCOC(=O)C1=C(NN=C(C)C)C2=C(N=C1)N(CC)N=C2
InChI
InChIKey=GQJUGJHJUZSJLZ-UHFFFAOYSA-N
InChI=1S/C14H19N5O2.ClH/c1-5-19-13-10(8-16-19)12(18-17-9(3)4)11(7-15-13)14(20)21-6-2;/h7-8H,5-6H2,1-4H3,(H,15,18);1H
Etazolate (EHT-0202) is a selective, positive GABAA receptor modulator has completed phase II clinical trials in patients with Alzheimer's disease. It is also a selective phosphodiesterase-4 inhibitor that is specific for cAMP. Etazolate showed anxiolytic and antidepressant activity and could be useful in managing post-traumatic stress disorder.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: CHEMBL2093872 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18397369 |
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Target ID: CHEMBL2093863 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23384434 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Interaction of allosteric ligands with GABAA receptors containing one, two, or three different subunits. | 1996 Apr 22 |
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Global expression profiling of theophylline response genes in macrophages: evidence of airway anti-inflammatory regulation. | 2005 Aug 8 |
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Etazolate, a neuroprotective drug linking GABA(A) receptor pharmacology to amyloid precursor protein processing. | 2008 Jul |
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A cell protection screen reveals potent inhibitors of multiple stages of the hepatitis C virus life cycle. | 2010 Feb 23 |
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EHT0202 in Alzheimer's disease: a 3-month, randomized, placebo-controlled, double-blind study. | 2011 Mar |
Patents
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT00880412
2 capsules of study treatment (capsules of EHT0202 (ETAZOLATE) 40mg and or 80mg and/or placebo) are taken twice a day during breakfast and dinner over a 3-month treatment period.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18397369
Etazolate (20 nM-2 microM) dose-dependently protected rat cortical neurons against Abeta-induced toxicity. The neuroprotective effects of etazolate were fully blocked by GABA(A) receptor antagonists indicating that this neuroprotection was due to GABA(A) receptor signalling
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C28197
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CHEMBL356388
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ACTIVE MOIETY
SUBSTANCE RECORD