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Details

Stereochemistry ACHIRAL
Molecular Formula C14H19N5O2
Molecular Weight 289.333
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of ETAZOLATE

SMILES

CCOC(=O)C1=CN=C2N(CC)N=CC2=C1NN=C(C)C

InChI

InChIKey=OPQRBXUBWHDHPQ-UHFFFAOYSA-N
InChI=1S/C14H19N5O2/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)

HIDE SMILES / InChI

Molecular Formula C14H19N5O2
Molecular Weight 289.333
Charge 0
Count
MOL RATIO 1 MOL RATIO (average)
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description

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.

Originator

Approval Year

Targets

Primary TargetPharmacologyConditionPotency

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
Unknown

Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer



Drug as perpetrator​

PubMed

Patents

Sample Use Guides

In Vivo Use Guide
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
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
Record UNII
I89Y79062L
Record Status Validated (UNII)
Record Version