Flumazenil decreases surface expression of α4β2δ GABAA receptors by increasing the rate of receptor internalization.

@article{Kuver2016FlumazenilDS,
  title={Flumazenil decreases surface expression of α4β2δ GABAA receptors by increasing the rate of receptor internalization.},
  author={Aarti Kuver and Sheryl Sue Smith},
  journal={Brain research bulletin},
  year={2016},
  volume={120},
  pages={131-43}
}
Increases in expression of α4βδ GABAA receptors (GABARs), triggered by fluctuations in the neurosteroid THP (3α-OH-5α[β]-pregnan-20-one), are associated with changes in mood and cognition. We tested whether α4βδ trafficking and surface expression would be altered by in vitro exposure to flumazenil, a benzodiazepine ligand which reduces α4βδ expression in vivo. We first determined that flumazenil (100 nM-100 μM, IC50=∼1 μM) acted as a negative modulator, reducing GABA (10 μM)-gated current in… CONTINUE READING
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