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EVT-201 ATC code
7-Chloro-3-{5-[(dimethylamino)methyl]-1,2,4-oxadiazol-3-yl}-5-methyl-4,5-dihydro-6H -imidazo[1,5-a ][1,4]benzodiazepin-6-one
CAS Number PubChem CID ChemSpider Formula C 17 H 17 Cl N 6 O 2 Molar mass 372.809 g/mol g·mol−1 3D model (JSmol )
Clc4cccc3n2cnc(c1nc(on1)CN©C)c2CN(C(=O)c34)C
InChI=1S/C17H17ClN6O2/c1-22(2)8-13-20-16(21-26-13)15-12-7-23(3)17(25)14-10(18)5-4-6-11(14)24(12)9-19-15/h4-6,9H,7-8H2,1-3H3
Key:JCYLWUVDHLVGER-UHFFFAOYSA-N
EVT-201 is a benzodiazepine derivative drug and partial positive allosteric modulator of the benzodiazepine site of the GABAA receptor .[ 1] It has 2–4-fold higher functional affinity for the α1 subunit relative to the α2 , α3 , and α5 subunits and significantly less intrinsic activity in comparison to currently-marketed benzodiazepines and the Z-drugs .[ 2] Despite the lower efficacy, EVT-201 still shows effectiveness in the treatment of insomnia , and it is thought that the lower efficacy may result in fewer side effects , such as motor incoordination .[ 2] The drug was originally developed by Roche , based on preclinical data, as a non-sedating anxiolytic , but was found to produce sedation in humans in phase I clinical trials . For this reason, it was subsequently licensed to Evotec , which is now developing it for the treatment of insomnia.[ 2] As of 2007, EVT-201 has completed phase II clinical trials for this indication, with positive findings reported.[ 3] As of August, 2015, Phase II development is ongoing in China .[ 4]
References
GABAA receptor positive modulators
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