神经药理学报

神经药理学报 ›› 2022, Vol. 12 ›› Issue (3): 1-.DOI: 10.3969/j.issn.2095-1396.2022.03.001

• 研究论文 •    下一篇

5-HT2A/D2 受体平衡拮抗剂NH809抗精神分裂症作用的初步研究

于民权，徐祥清   

  1. 江苏恩华药业股份有限公司，徐州，221000，中国
  • 出版日期:2022-06-26 发布日期:2022-06-26
  • 作者简介:于民权，硕士研究生；研究方向：主要从事神经精神药理学研究；E-mail：yuminquan@126.com

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

YU Min-quan，XU Xiang-qing   

  1. Jiangsu Nhwa Pharmaceutical Co.，Ltd，Xuzhou，221000，China
  • Online:2022-06-26 Published:2022-06-26

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摘要： 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。

关键词: 5-HT2A/D2 受体平衡拮抗剂, 高活动, 攀爬, 条件回避

Abstract:

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.

Key words: 5-HT2A/D2 receptor balance antagonist, hyperactivity, climbing behavior, CAR

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