PNU-107484A is a selective GABAA receptor ligand with distinct activity across various α isoform subtypes. It functions as a positive allosteric modulator for the α1β2γ2 subtype, enhancing GABA-induced chloride currents, while exhibiting inhibitory effects on the α3β2γ2 and α6β2γ2 subtypes. The compound demonstrates half-maximal inhibitory concentrations of 3.1 μM for α1β2γ2, 4.2 μM for α3β2γ2, and 3.5 μM for α6β2γ2. PNU-107484A serves as a valuable tool for exploring the physiological implications of different GABAA receptor α isoform subtypes in research settings.
PNU-107484A is a selective GABAA receptor ligand with distinct activity across various α isoform subtypes. It functions as a positive allosteric modulator for the α1β2γ2 subtype, enhancing GABA-induced chloride currents, while exhibiting inhibitory effects on the α3β2γ2 and α6β2γ2 subtypes. The compound demonstrates half-maximal inhibitory concentrations of 3.1 μM for α1β2γ2, 4.2 μM for α3β2γ2, and 3.5 μM for α6β2γ2. PNU-107484A serves as a valuable tool for exploring the physiological implications of different GABAA receptor α isoform subtypes in research settings.
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