GL-II-73 explained
GL-II-73 (GL-ii-073) is a benzodiazepine derivative related in chemical structure to compounds such as midazolam and adinazolam. 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] [5] [6] [7]
See also
Notes and References
- CA . 3016491 . Cook JM, Li G, Poe M, Savic M, Sibille E . Centre for Addiction and Mental Health, Faculty Of Pharmacy, University of Belgrade . UWM Res Foundation Inc . Treatment of cognitive and mood symptoms in neurodegenerative and neuropsychiatric disorders with alpha5-containing gabaa receptor agonists. . 21 September 2017 .
- Prevot TD, Li G, Vidojevic A, Misquitta KA, Fee C, Santrac A, Knutson DE, Stephen MR, Kodali R, Zahn NM, Arnold LA . 90987308 . Potential combined pro-cognitive, anxiolytic and antidepressant properties of novel GABAA receptor positive modulators with preferential efficacy at the α5-subunit. . bioRxiv . January 2018 . 332908 . 10.1101/332908 .
- Prevot TD, Li G, Vidojevic A, Misquitta KA, Fee C, Santrac A, Knutson DE, Stephen MR, Kodali R, Zahn NM, Arnold LA, Scholze P, Fisher JL, Marković BD, Banasr M, Cook JM, Savic M, Sibille E . Novel Benzodiazepine-Like Ligands with Various Anxiolytic, Antidepressant, or Pro-Cognitive Profiles . Molecular Neuropsychiatry . 5 . 2 . 84–97 . April 2019 . 31192221 . 6528097 . 10.1159/000496086 .
- Web site: Brain Inhibitory GABAergic Function and Cognitive Deficits: Mechanisms and Therapeutic Targeting. . Etienne . Sibille . Presentation for AAAS . February 2019 . 2019-03-09 . 2019-04-12 . https://web.archive.org/web/20190412041410/https://www.sibillelab.com/wp-content/uploads/2019/02/AAAS-Sibille.pdf . dead .
- Maramai S, Benchekroun M, Ward SE, Atack JR . Subtype Selective γ-Aminobutyric Acid Type A Receptor (GABAAR) Modulators Acting at the Benzodiazepine Binding Site: An Update . Journal of Medicinal Chemistry . 63 . 7 . 3425–3446 . April 2020 . 10.1021/acs.jmedchem.9b01312 . 31738537 . 208171129 .
- Bernardo A, Lee P, Marcotte M, Mian MY, Rezvanian S, Sharmin D, Kovačević A, Savić MM, Cook JM, Sibille E, Prevot TD . Symptomatic and neurotrophic effects of GABAA receptor positive allosteric modulation in a mouse model of chronic stress . Neuropsychopharmacology . 47 . 9 . 1608–1619 . August 2022 . 10.1038/s41386-022-01360-y . 35701547 . 9283409 .
- Perez SM, McCoy AM, Prevot TD, Mian MY, Carreno FR, Frazer A, Cook JM, Sibille E, Lodge DJ . Hippocampal α5-GABAA Receptors Modulate Dopamine Neuron Activity in the Rat Ventral Tegmental Area . Biological Psychiatry Global Open Science . 3 . 1 . 78–86 . January 2023 . 10.1016/j.bpsgos.2021.12.010 . 36712569 . 9874136 .