CGP 7930 is a positive allosteric modulator of GABAA and GABAB receptors. Increases the potency and efficacy of GABA at both recombinant and native GABAB receptors (EC50 values are 4.60 μM and 5.37 μM respectively) and enhances the inhibitory effect of the agonist L-baclofen in cultured cortical neurons. In HEK-293 cells expressing recombinant GABAA receptor, CGP 7930 increases the potency and efficacy of GABA (EC50 values are 1.0 μM and 1.7 μM at α4β3δ and α1β2γ2L receptors respectively). In cultured hippocampal neurons, pre-application of CGP 7930 causes concentration-dependent potentiation of GABAA receptor currents by specific type-A receptor agonist Muscimol (EC50 = 2.0 μM). CGP7930 potentiates GABAA receptor-mediated tonic inhibition, reduces the frequency of inhibitory postsynaptic currents and prolongs rise and decay times. CGP 7930 also blocks G protein-coupled inwardly rectifying K+ (GIRK) channels diminishing GABAA receptor signaling in HEK 293 cells. CGP 7930 reduces operant self-administration of ethanol in alcohol-preferring rats following i.p. administration.
