最小反应模型分析丙戊酸钠抗脑NMDA受体  

Analysis of the effect of valprorate sodium on brain N-methyl-D-aspartate receptor on minimal reaction model

作　　者：顾饶胜[1] 陈厚昌[1,2] 何玲[1] 陈厚昌[1,2] 蒋毅萍 

机构地区：[1]空军医学高等专科学校,吉林市132013 [2]解放军第一军医大学,广州市510515

出　　处：《空军医高专学报》1998年第4期187-190,共4页

摘　　要：为进一步研究丙戊酸钠（VPA）对脑N-甲基-D-天门冬氨酸（NMDA）受体的作用机制,将大鼠脑NMDA受体的mRNA注入非洲爪蟾卵母细胞,表达出相应的功能性NMDA受体,以全细胞电压钳位法和快速全细胞灌流法测定不同浓度NMDA激活NMDA受体产生的内向跨膜电流,分析VPA对NMDA受体的拮抗作用,并与DAP（DL-α,ε-diaminopimelic acid）的拮抗作用比较,以最小反应模型分析VPA抗NMDA受体的作用机制。结果表明,以竞争性拮抗模型和非竞争性拮抗模型分析VPA的拮抗作用所得K值分别为0.042mmol/L和0.089mmol/L,DAP的K值分别为0.076mmol/L和0.165mmol/L;两者均与竞争性拮抗模型的配合程度较好,与非竞争性拮抗模型的配合程度较差,由此推论,VPA对NMDA受体的直接作用与DAP相似,属于竞争性拮抗作用。To study the action of valprorate sodiu m(VPA) on NMDA receptor, the inward membrane currents of oocytes injected with neonatal rat brain mRNA induced by various concentrations of NMDA and effect of VPA and DAP (DL-α, ε-diaminopielic acid) on current were measured with voltage clamp technique. The actions of VPA and DAP on NMDA receptor were analyzed by using the minimal reaction model. The results (K = 0.076 mmol/L and 0.165 mmol/L for DAP, K = 0.042 mmol/L and 0.089 mmol/L for VPA) were obtained by using the competitive antagonistic model and the noncompetitive antagonistic model. The good fit of experimental data to the equation for competitive antagonistic model rather than for the noncompetitive antagonistic model indicates that both VPA and DAP are competitive antagonists to NMDA receptor.

关 键 词：丙戊酸钠 最小反应模型 受体 

分 类 号：R742.1[医药卫生—神经病学与精神病学]