Evt-201
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Grundinformationen
- CAS
308239-86-3- Standard-SMILES
CN(C)Cc1nc(-c2ncn3c2CN(C)C(=O)c2c(Cl)cccc2-3)no1- InChIKey
JCYLWUVDHLVGER-UHFFFAOYSA-N- Summenformel
- C17H17ClN6O2
- Durchschnittliche Molmasse
- 372,8 g/mol
- Monoisotopische Masse
- 372,1101515
Namen und Bezeichner
- Bevorzugter Name
- Evt-201
- IUPAC
- 7-chloro-3-[5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl]-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-one
Namen und Synonyme
EVT-201308239-86-3EVT2016J8AF7CLE4EVT 201DTXSID3010320556H-Imidazo[1,5-a][1,4]benzodiazepin-6-one, 7-chloro-3-[5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl]-4,5-dihydro-5-methyl-6H-IMIDAZO(1,5-A)(1,4)BENZODIAZEPIN-6-ONE, 7-CHLORO-3-(5-((DIMETHYLAMINO)METHYL)-1,2,4-OXADIAZOL-3-YL)-4,5-DIHYDRO-5-METHYL-RefChem:596970DTXCID8015170581198427-03-0Dimdazenil
Weitere Namen anzeigen
7-chloro-3-[5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl]-5-methyl-4H-imidazo[1,5-a][1,4]benzodiazepin-6-oneDimdazenil (INN)Dimdazenil [INN]JunoenilDimdazenil [WHO-DD]UNII-6J8AF7CLE4SCHEMBL3088188CHEMBL5095096
Datenbank-Bezeichner
- CAS
308239-86-3- PubChem CID
- 9885841
- DTXSID
DTXSID301032055- ChEMBL
CHEMBL5095096- UNII
- 6J8AF7CLE4
Eigenschaften
Berechnete StruktureigenschaftenWird ergänzt
- XLogP
- 1,2
- Polarare Oberfläche (TPSA)
- 80,3 Ų
- H-Brücken-Donoren
- 0
- H-Brücken-Akzeptoren
- 6
- Frei drehbare Bindungen
- 3
- Schwere Atome
- 26
- Formalladung
- 0
- Komplexität
- 537
Chemie und Industrie
Pharmakologische Informationen
ATC CodeN - Nervous system；N05 - Psycholeptics；N05C - Hypnotics and sedatives；N05CD - Benzodiazepine derivatives；N05CD16 - Dimdazenil
Pharmacodynamics
In two Phase I/II studies using the traffic noise model of insomnia in healthy male volunteers, EVT 201 significantly reduced "wake after sleep onset" (WASO) while significantly increasing "total sleep time" (TST) and quality of sleep with no subjective residual effects. The compound was well tolerated without significant adverse events.
Mechanism of Action
EVT 201 is a partial positive allosteric modulator (pPAM) of the GABAA receptor complex and consequently works through a proven pathway in the treatment of insomnia. However, EVT 201’s partial agonist activity gives it a differentiated pre-clinical profile and mechanism of action compared to many currently marketed sleep-promoting agents.
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