General
Preferred name
ETIZOLAM
Synonyms
Y-7131 ()
AHR 3219 ()
Etizolam RM ()
Etizolam (CRM) ()
DEA NO. 2780 ()
Sedekopan ()
Etizolam-d4 ()
P&D ID
PD009014
CAS
40054-69-1
Tags
available
drug
First approval
1984
Drug Status
approved
experimental
investigational
Max Phase
2.0
Drug indication
Anxiety
Structure
Probe scores
P&D probe-likeness score
[[ v.score ]]%
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
PHARMACODYNAMICS Etizolam is a CNS depressant with anxiolytic, anticonvulsant, sedative-hypnotic and muscle relaxant effects. It acts on the benzodiazepine site of the GABA-A receptor as an agonist to increase inhibitory GABAergic transmission throughout the central nervous system. Studies indicate that etizolam mediates its pharmacological actions with 6 to 10 times more potency than that of diazepam. Clinical human studies performed in Italy showed clinical effectiveness of etizolam in relieving symptoms in patients with generalized anxiety disorders with depressive symptoms [A19772, A19773, A19774]. Etizolam also mediates imipramine-like neuropharmacological and behavioral effects, as well as minor effects on cognitive functioning. It is shown to substitute the actions of a short-acting barbiturate, pentobarbitol, in a drug discrimination study [L883]. ; Etizolam is an antagonist at platelet-activating-factor (PAF) receptor and attenuates the recurrence of chronic subdural hematoma after neurosurgery in clinical studies [L884]. It is shown to inhibit PAF-induced bronchoconstriction and hypotension [A19775].
MOA Etizolam is selectively a full agonist at GABA-A receptors to increase GABAergic transmission and enhance GABA-induced Cl- currents [A19771]. It is reported to bind to the benzodiazepine binding site which is located across the interface between the alpha and gamma subunits. Benzodiazapines are reported to only bind to receptors that contain gamma 2 and alpha 1/2/3/5 subunits [T28]. Alpha-1-containing receptors mediate the sedative effects of etizolam whereas alpha-2 and alpha-3 subunit-containing receptors mediate the anxiolytic effect [T28]. Etizolam shows high potency and affinity towards GABA-A receptor with alpha 1 beta 2 gamma 2S subunit combination [A19771]. By binding to the regulatory site of the receptor, etizolam potentiates GABA transmission by facilitating the opening of GABA-induced chloride channels [T28].; Etizolam is a specific antagonist at PAFR. It inhibits PAF-induced platelet aggregation by inhibiting PAF binding to the receptors located on the surface of platelets with an IC50 of 22nM [A19775].
Compound Sets
10
AdooQ Bioactive Compound Library
A14257
Cayman Chemical Bioactives
12063
20991
38190
ChEMBL Drugs
CHEMBL1289779
Drug Repurposing Hub
DrugBank
DB09166
DrugCentral
1102
DrugCentral Approved Drugs
1102
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
ReFrame library
External IDs
24
Properties
(calculated by RDKit )
Molecular Weight
342.07
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
0
Rotatable Bonds
2
Ring Count
4
Aromatic Ring Count
3
cLogP
4.2
TPSA
43.07
Fraction CSP3
0.24
Chiral centers
0.0
Largest ring
7.0
QED
0.7
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
platelet-activating factor (PAF)
GABRA1
MOA
Platelet aggregation Inhibitor
GABA(A) BZ Site Receptor Agonists
Platelet-Activating Factor Receptor (PAFR) Antagonists
benzodiazepine receptor agonist
Member status
virtual
Indication
insomnia, anxiety
Source data