5-HT2A/D2 受体平衡拮抗剂NH809抗精神分裂症作用的初步研究

目的：考察5-HT2A/D2 受体平衡拮抗剂NH809 体内抗精神分裂症药理学作用。方法：采用地卓西平马来酸盐（0.3 mg·kg^-1，ip）诱发小鼠高活动模型、阿扑吗啡（1 mg·kg^-1，sc）诱导小鼠攀爬模型及大鼠条件回避反应（conditioned avoidance response，CAR）实验，评估NH809 体内抗精神分裂症的作用，并与阳性药利培酮进行比较。结果：在地卓西平马来酸盐诱发小鼠高活动模型、阿扑吗啡诱导小鼠攀爬行为及大鼠条件回避反应体内动物 模型上，NH809 具有剂量相关的抑制作用，其ED50 分别为0.04、0.05 和0.24 mg·kg^-1；利培酮在这三个模型上的ED50 分别为0.06、0.68 和0.60 mg·kg^-1。结论：NH809 对多个精神分裂症动物模型具有显著的药理学作用，且体内活性优于利培酮。

A Preliminary Study on the Effect of 5-HT2A/D2 Receptor Balancing Antagonist NH809 on Schizophrenia

Objective：To investigate the pharmacological effects of 5-HT2A/D2 receptor balancing antagonist NH809 on schizophrenia in vivo. Methods：The effects of NH809 on schizophrenia in vivo were evaluated by MK-801 hydrogen maleat（0.3 mg·kg^-1，ip） induced hyperactivity model in mice，apomorphine （1 mg·kg^-1，sc） induced climbing model in mice and conditioned avoidance response（CAR） in rats，and compared with risperidone. Results：NH809 had dose-dependent inhibitory effect on MK-801 hydrogen maleate induced high activity model，apomorphine-induced climbing behavior in mice and conditioned avoidance response in vivo，with ED50 of 0.04，0.05 and 0.24 mg·kg^-1，respectively. The ED50 of risperidone in these three models were 0.06，0.68 and 0.60 mg·kg^-1，respectively. Conclusion：NH809 has significant pharmacological effects on several animal models of schizophrenia，and its activity in vivo is better than risperidone.