A GABAB receptors antagonist; selectively reverses (-)-baclofen-induced inhibition of potassium-evoked GABA release over glutamate or somatostatin release (IC50s = 0.085, 3.35, and 9.26 μM, respectively) from rat cortical synaptosomes; reduces paired-pulse inhibition of IPSPs by 80% in CA1 pyramidal neurons in rat hippocampal slices at 10 μM; increases cell proliferation in the ventral subgranular zone of the dentate gyrus when administered at a dose of 3 mg/kg per day for 21 days and reduces immobility in the forced-swim test when administered at 10 mg/kg in stress-sensitive BALB/c mice; inhibits the analgesic effects of isovaline, GABA, and baclofen in a mouse model of hindpaw allodynia induced by PGE2