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
Molecular Formula | C14H19N5O2 |
Molecular Weight | 289.333 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Molecular Formula | ClH |
Molecular Weight | 36.461 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
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 |
---|---|---|---|
Target ID: CHEMBL2093872 Sources: https://www.ncbi.nlm.nih.gov/pubmed/18397369 |
|||
Target ID: CHEMBL2093863 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23384434 |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | Unknown Approved UseUnknown |
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
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:16:34 GMT 2023
by
admin
on
Fri Dec 15 15:16:34 GMT 2023
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Record UNII |
7YO3254Y6B
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C28197
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35838-58-5
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37274
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C72768
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CHEMBL356388
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |