2133456-91-2
Chemical Structure
GL-II-73
- CAS No.: 2133456-91-2
- Formula:C23H19FN4O
- Molecular Weight:386.42
InChIKey: LNPOWXXHIUMIKI-CQSZACIVSA-N
SMILES: O=C(C1=C2N(C=N1)C3=CC=C(C#C)C=C3C(C4=CC=CC=C4F)=N[C@@H]2C)N(C)C
Biological Activity: GL-II-73 is a selective, orally active and blood-brain barrier permeable positive allosteric modulator of α5GABAA receptor, acting on the benzodiazepine-binding site of GABAA receptors. The binding selectivity of GL-II-73 for the α5 subtype is 6-, 11- and 12.5-fold higher than that for the α2, α1 and α3 subtypes, respectively. GL-II-73 reverses pilocarpine-induced hyperactivation of dopamine neurons in the ventral tegmental area, improves working memory and pyramidal neuron dendritic morphology in 5xFAD mice, but does not reduce β-amyloid load. GL-II-73 can be used in research related to Alzheimer's disease and temporal lobe epilepsy with comorbid psychosis[2][3].
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GL-II-73 | GL-II-73 is a selective, orally active and blood-brain barrier permeable positive allosteric modulator of α5GABAA receptor, acting on the benzodiazepine-binding site of GABAA receptors. The binding selectivity of GL-II-73 for the α5 subtype is 6-, 11- and 12.5-fold higher than that for the α2, α1 and α3 subtypes, respectively. GL-II-73 reverses pilocarpine-induced hyperactivation of dopamine neurons in the ventral tegmental area, improves working memory and pyramidal neuron dendritic morphology in 5xFAD mice, but does not reduce β-amyloid load. GL-II-73 can be used in research related to Alzheimer's disease and temporal lobe epilepsy with comorbid psychosis. | |||||||||||||||||||||
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- [2]. Bernardo AM, et al. Procognitive and neurotrophic benefits of α5-GABA-A receptor positive allosteric modulation in a β-amyloid deposition mouse model of Alzheimer's disease pathology. Neurobiology of aging. 2025 Mar;147:49-59. [Content Brief]
- [3]. McCoy AM, Prevot TD, Sharmin D, Cook JM, Sibille EL, Lodge DJ. GL-II-73, a Positive Allosteric Modulator of α5GABAA Receptors, Reverses Dopamine System Dysfunction Associated with Pilocarpine-Induced Temporal Lobe Epilepsy. Int J Mol Sci. 2023;24:11588. [Content Brief]
Keywords
