5-HT_(2A)/D_(2)受体平衡拮抗剂NH809抗精神分裂症作用的初步研究  

A Preliminary Study on the Effect of5-HT_(2A)/D_(2)Receptor Balancing Antagonist NH809 on Schizophrenia

作　　者：于民权[1] 徐祥清[1] YU Min-quan;XU Xiang-qing(Jiangsu Nhwa Pharmaceutical Co.,Ltd,Xuzhou,221000,China)

机构地区：[1]江苏恩华药业股份有限公司,徐州221000

出　　处：《神经药理学报》2022年第3期1-4,共4页Acta Neuropharmacologica

摘　　要：目的:考察5-HT_(2A)/D_(2)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ED_(50)分别为0.04、0.05和0.24 mg·kg^(-1);利培酮在这三个模型上的ED_(50)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。Objective:To investigate the pharmacological effects of 5-HT_(2A)/D_(2)receptor balancing antagonist NH809 on schizophrenia in vivo.Methods:The effects of NH809 on schizophrenia in vivo were evaluated by MK-801 hydrogen maleate(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 ED_(50) of 0.04,0.05 and 0.24 mg·kg^(-1),respectively.The ED_(50) 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.

关 键 词：5-HT2A/D2受体平衡拮抗剂 高活动 攀爬 条件回避 

分 类 号：R749.3[医药卫生—神经病学与精神病学]