DGIdb - ESZOPICLONE Drug Record

ESZOPICLONE chembl:CHEMBL1522 Approved

Alternate Names:

ESZOPICLONE
(S)-ZOPICLONE
ZOPICLONE S-FORM
GSK-1755165
LUNESTA
ESZOPICLONE CIV
(+)-ZOPICLONE
(+)-(5S)-6-(5-CHLOROPYRIDIN-2-YL)-7-OXO-6,7-DIHYDRO-5H-PYRROLO(3,4-B)PYRAZIN-5-YL 4-METHYLPIPERAZINE-1-CARBOXYLATE
(S)-6-(5-CHLORO-2-PYRIDINYL)- 7-OXO- 6,7-DIHYDRO- 5H-PYRROLO[3,4-B]PYRAZIN-5-YL- 4-METHYL- 1-PIPERAZINECARBOXYLATE
1-PIPERAZINECAROBXYLIC ACID,4-METHYL-,(5S)-6-(5-CHLORO-2-PYRIDINYL)-6,7-DIHYDRO-7-OXO-5H-PYRROLO[3,4-B]PYRAZIN-5-YL ESTER
ESTORRA
LUNESTA®
ESOPICLONE
(+)-(5S)-6-(5-CHLOROPYRIDIN-2-YL)-7-OXO-6,7-DIHYDRO-5H-PYRROLO[3,4-B]PYRAZIN-5-YL-4-METHYLPIPERAZINE-1-CARBOXYLATE
chemidplus:138729-47-2
pubchem.compound:969472
chembl:CHEMBL1522
drugbank:00402
rxcui:461016

Drug Info:

Drug Indications	anxiolytic
FDA Approval	approved
Drug Class	Small molecule
Drug Indications	hypnotic

(1 More Sources)

Publications:

Nutt et al., 2010, Searching for perfect sleep: the continuing evolution of GABAA receptor modulators as hypnotics., J. Psychopharmacol. (Oxford)
Hanson et al., 2008, Structural requirements for eszopiclone and zolpidem binding to the gamma-aminobutyric acid type-A (GABAA) receptor are different., J. Med. Chem.
Wadworth AN et al., 1993, Zopiclone. A review of its pharmacological properties and therapeutic efficacy as an hypnotic., Drugs Aging
Dixon CL et al., 2015, Zolpidem and eszopiclone prime α1β2γ2 GABAA receptors for longer duration of activity., Br J Pharmacol
Döble A et al., 1995, The mechanism of action of zopiclone., Eur Psychiatry
Becker et al., 2009, Treatment of sleep dysfunction and psychiatric disorders., Curr Treat Options Neurol
Jufe, [New hypnotics: perspectives from sleep physiology]., Vertex
Imming et al., 2006, Drugs, their targets and the nature and number of drug targets., Nat Rev Drug Discov
Overington et al., 2006, How many drug targets are there?, Nat Rev Drug Discov
Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

ESZOPICLONE TSPO

Interaction Score: 0.61

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lunesta

PMIDs:
19744401 18265473 17016423 17139284

Sources:
TdgClinicalTrial TTD
ESZOPICLONE GABRA1

Interaction Score: 0.26

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Trial Name Lunesta

PMIDs:
19942638 18973287 8241608 25817320 19698408

Sources:
TdgClinicalTrial ChemblInteractions
ESZOPICLONE GABRA5

Interaction Score: 0.19

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name Lunesta

PMIDs:
19942638 18973287

Sources:
TdgClinicalTrial ChemblInteractions
ESZOPICLONE GABRA3

Interaction Score: 0.18

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lunesta

Direct Interaction yes

PMIDs:
19942638 18973287

Sources:
TdgClinicalTrial ChemblInteractions
ESZOPICLONE GABRA2

Interaction Score: 0.18

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Trial Name Lunesta

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
19942638 18973287

Sources:
TdgClinicalTrial ChemblInteractions
ESZOPICLONE CYP3A5

Interaction Score: 0.07

Interaction Types & Directionality:

n/a

Interaction Info:

PMIDs:
18695978

Sources:
PharmGKB
ESZOPICLONE GABRQ

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRE

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRP

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRD

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRB3

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRG1

Interaction Score: 0.06

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRB1

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRA4

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRG2

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRA6

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRB2

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions
ESZOPICLONE GABRG3

Interaction Score: 0.05

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions

TdgClinicalTrial: ESZOPICLONE
- Version: January-2014
Alternate Names:

Drug Info:

Drug Indications hypnotic

Drug Class Small molecule

FDA Approval approved

Publications:
PharmGKB: eszopiclone
- Version: 18-August-2020
Alternate Names:

Drug Info:

Publications:

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem
TTD: Eszopiclone
- Version: 2020.06.01
Alternate Names:

D06ZII TTD Drug ID

Drug Info:

Publications:
ChemblDrugs: chembl:CHEMBL1522
- Version: ChEMBL_27
Alternate Names:

Drug Info:

Publications:
ChemblInteractions: CHEMBL1522
- Version: chembl_23
Alternate Names:

Drug Info:

Publications:

Direct Interaction	yes
Mechanism of Interaction	GABA-A receptor; anion channel positive allosteric modulator
Trial Name	Lunesta

Novel drug target	Established target
Trial Name	Lunesta
Direct Interaction	yes

positive modulator (activating)
potentiator

positive modulator (activating)
agonist (activating)

positive modulator (activating)
agonist (activating)

positive modulator (activating)
agonist (activating)

ESZOPICLONE Drug Record

ESZOPICLONE chembl:CHEMBL1522 Approved

Alternate Names:

Drug Info:

Publications:

Interaction Types & Directionality: agonist (activating)

Interaction Info: Novel drug target Established target Trial Name Lunesta

PMIDs: 19744401 18265473 17016423 17139284

Sources: TdgClinicalTrial TTD

Interaction Types & Directionality: positive modulator (activating) potentiator

Interaction Info: Direct Interaction yes Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Trial Name Lunesta

PMIDs: 19942638 18973287 8241608 25817320 19698408

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: positive modulator (activating) agonist (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes Trial Name Lunesta

PMIDs: 19942638 18973287

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: positive modulator (activating) agonist (activating)

Interaction Info: Novel drug target Established target Trial Name Lunesta Direct Interaction yes

PMIDs: 19942638 18973287

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: positive modulator (activating) agonist (activating)

Interaction Info: Trial Name Lunesta Novel drug target Established target Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs: 19942638 18973287

Sources: TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality: n/a

Interaction Info:

PMIDs: 18695978

Sources: PharmGKB

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator Direct Interaction yes

PMIDs: None found

Sources: ChemblInteractions

Interaction Types & Directionality: positive modulator (activating)

Interaction Info: Direct Interaction yes Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs: None found

Sources: ChemblInteractions

TdgClinicalTrial: ESZOPICLONE

Alternate Names:

Drug Info: Drug Indications hypnotic Drug Class Small molecule FDA Approval approved

Interaction Types & Directionality:

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lunesta

PMIDs:
19744401 18265473 17016423 17139284

Sources:
TdgClinicalTrial TTD

Interaction Types & Directionality:

positive modulator (activating)

potentiator

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Trial Name Lunesta

PMIDs:
19942638 18973287 8241608 25817320 19698408

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

Trial Name Lunesta

PMIDs:
19942638 18973287

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Novel drug target Established target

Trial Name Lunesta

Direct Interaction yes

PMIDs:
19942638 18973287

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

agonist (activating)

Interaction Info:

Trial Name Lunesta

Novel drug target Established target

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
19942638 18973287

Sources:
TdgClinicalTrial ChemblInteractions

Interaction Types & Directionality:

n/a

PMIDs:
18695978

Sources:
PharmGKB

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

Direct Interaction yes

PMIDs:
None found

Sources:
ChemblInteractions

Interaction Types & Directionality:

positive modulator (activating)

Interaction Info:

Direct Interaction yes

Mechanism of Interaction GABA-A receptor; anion channel positive allosteric modulator

PMIDs:
None found

Sources:
ChemblInteractions

Drug Info:

Drug Indications hypnotic

Drug Class Small molecule

FDA Approval approved

Publications:

Zanger UM et al., 2008, Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformation., Anal Bioanal Chem

Alternate Names:

D06ZII TTD Drug ID