Cayman CGP 52432

CGP 52432 is an antagonist of GABA_B receptors. It 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. CGP 52432 (10 μM) reduces paired-pulse inhibition of monosynaptic inhibitory potentials (IPSPs) by 80% in CA1 pyramidal neurons in rat hippocampal slices. It 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. CGP 52432 (30 mg/kg) increases locomotor activity in mice. It also inhibits the analgesic effects of isovaline, GABA, and baclofen (Item No. ) in a mouse model of hindpaw allodynia induced by prostaglandin E₂ (PGE₂; Item No. ).

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