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GL-II-73
(4R)-8-ethynyl-6-(2-fluorophenyl)-N,N,4-trimethyl-4H-benzo[f]imidazo[1,5-a] [1,4]diazepine-3-carboxamide
PubChem CID Formula C 23 H 19 F N 4 O Molar mass −1 3D model (JSmol )
CN(C)C(=O)c4ncn2c4[C@@H](C)N=C(c1cc(C#C)ccc12)c3ccccc3F
InChI=1S/C23H19FN4O/c1-5-15-10-11-19-17(12-15)20(16-8-6-7-9-18(16)24)26-14(2)22-21(23(29)27(3)4)25-13-28(19)22/h1,6-14H,2-4H3/t14-/m1/s1
Key:LNPOWXXHIUMIKI-CQSZACIVSA-N
GL-II-73 (GL-ii-073 ) is a benzodiazepine derivative related in chemical structure to compounds such as midazolam , adinazolam and the active metabolite of rilmazafone . It is described as an α5 preferring positive allosteric modulator of the benzodiazepine site of GABAA receptors , with weaker activity at α2 and α3 and no significant affinity for the α1 subtype. In animal tests it was found to produce effects consistent with antidepressant , anxiolytic and nootropic actions.[ 1] [ 2] [ 3] [ 4]
See also
References
^ Cook JM, Li G, Poe M, Savic M, Sibille E. Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with alpha5-containing gabaa receptor agonists. Patent application CA3016491
^ Prevot TD, et al. Potential combined pro-cognitive, anxiolytic and antidepressant properties of novel GABAA receptor positive modulators with preferential efficacy at the α5-subunit. BioRxiv 2018 doi :10.1101/332908
^ Prevot TD, et al. Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles. Molecular Neuropsychiatry , 2019; 1. doi :10.1159/000496086
^ Etienne Sibille. Brain Inhibitory GABAergic Function and Cognitive Deficits: Mechanisms and Therapeutic Targeting. Presentation for AAAS, Feb 2019.
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