Positive modulation of synaptic and extrasynaptic GABAA receptors by an antagonist of the high affinity benzodiazepine binding site.
Positive modulation of synaptic and extrasynaptic GABAA receptors by an antagonist of the high affinity benzodiazepine binding site.
S. Middendorp,M. C. Maldifassi,R. Baur,E. Sigel
2015 · DOI: 10.1016/j.neuropharm.2015.04.027
Neuropharmacology · 20 Citations
TLDR
The compound SJM-3 was identified in a prospective screening of ligands for the benzodiazepine binding site and investigated for its site of action and was shown to act as an antagonist at the α+/γ- site and strongly potentiated GABA currents via the binding site for diazepam in the transmembrane domain.