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  6. Chronic Α5-gaba-a Receptor Potentiation Promotes Mouse Adult Hippocampal Neurogenesis

Chronic α5-GABA-A Receptor Potentiation Promotes Mouse Adult Hippocampal Neurogenesis

Thomas D Prevot1,2,3, Michael Marcotte1, Denis J David4

  • 1Campbell Family Mental Health Research Institute of CAMH, Toronto, Ontario, Canada.

Hippocampus|June 14, 2025

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View abstract on PubMed

Summary

A novel drug targeting the α5-GABAA receptor (α5-PAM) significantly boosted adult hippocampal neurogenesis (AHN) in mice. This effect, comparable to fluoxetine, involved increased cell proliferation, survival, and maturation of new neurons.

Area of Science:

  • Neuroscience
  • Cell Biology
  • Pharmacology

Background:

  • Adult hippocampal neurogenesis (AHN) is crucial for cognitive and mood-related behaviors.
  • Augmenting α5-γ-Aminobutyric acid type A (GABAA) receptor function shows promise for neurotrophic effects.
  • The impact of α5-GABAA receptor modulation on AHN is not well understood.

Purpose of the Study:

  • To investigate the effect of a novel α5-GABAA-R positive allosteric modulator (α5-PAM), GL-II-73, on adult mouse hippocampal neurogenesis.
  • To compare the impact of GL-II-73 on AHN with fluoxetine, a known enhancer of neurogenesis.

Main Methods:

  • Adult male mice were treated for 6 weeks with either GL-II-73 (α5-PAM) or fluoxetine.
  • Cell proliferation was assessed using Ki67.
  • Newborn neuron survival and maturation were evaluated using 5-Bromo-2´-Deoxyuridine (BrdU) retention and co-labeling with DCX and NeuN.

Main Results:

  • Chronic treatment with GL-II-73 significantly increased neuronal progenitor proliferation in the dentate gyrus (DG).
  • GL-II-73 enhanced the survival of adult-born granule cells.
  • The maturation rate of young adult-born neurons was also increased by GL-II-73 treatment.

Conclusions:

  • GL-II-73, an α5-GABAA-R positive allosteric modulator, effectively stimulates all stages of adult hippocampal neurogenesis.
  • The neurogenic effects of GL-II-73 are comparable to those of fluoxetine.
  • Targeting α5-GABAA receptors represents a potential therapeutic strategy for enhancing neurogenesis.
Keywords:
GABAadult hippocampal neurogenesisfluoxetinehippocampuspreclinicalα5‐γ‐aminobutyric acid type a (GABAA) receptor

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