CGP 52432

一种GABAB受体拮抗剂；选择性地逆转(-)-巴氯芬诱导的对大鼠皮质突触体中钾诱发的GABA释放的抑制，而不是谷氨酸或生长抑素释放（IC50s分别为0.085、3.35和9.26μM）；在10μM浓度下，可将大鼠海马切片中CA1锥体神经元中IPSP的配对脉冲抑制降低80%；在压力敏感的BALB/c小鼠中，以3mg/kg每天的剂量给药21天时，可增加齿状回腹侧颗粒下区的细胞增殖，以10mg/kg的剂量给药时，可降低强迫游泳测试中的不动性；在PGE2诱发的后爪异常性疼痛的小鼠模型中，抑制异缬氨酸、GABA和巴氯芬的镇痛作用。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.