Effect of sodium dimercaptopropanesulfonate on antagonism of tetramethylenedisulphotetramine to GABA receptor  

二巯丙磺钠对四次甲基二砜四胺拮抗GABA受体的影响(英文)

作　　者：张春颖[1] 朱桐君[1] 胡国新[1] 陈醒言[1] 刘鼎新[2,1] 刘鼎新 

机构地区：[1]温州医学院药理学教研室,温州中国325027 [2]北京医科大学细胞生物学教研室,北京中国100083

出　　处：《Acta Pharmacologica Sinica》2001年第5期55-59,共5页中国药理学报（英文版）

基　　金：Project supported by the Foundation from the Education Commission of Zhejiang Provence (990454)

摘　　要：AIM: To study effects of sodium dimercapto-propanesulfonate (DMPS) on the antagonism of tetram-ethylenedisulphotetramine (TETS) to μ-aminobutyric acid (GABA) receptor. METHODS: Acute toxicity experiments were conducted to observe the effects of DMPS and TETS on mice. Contents of free amino acids in mouse brain were determined with automatic analyzer for amino acids. Autoradiography was used to observe the [3H]GABA bindings in the rat brain slices under different conditions. RESULTS: After icv and ip DMPS, the number of mice experiencing convulsions reduced from 20 in control group to 4 and 2 respectively in TETS poisoned mice. The content of GABA was altered in DMPS control group and TETS control group compared with DMPS protection group and NS control group [μmol/g: (2.09 ±0.05) and (2.67 ±0.15) vs (2.40 ±0.10 (μmol/ g)) and (2.41 ±0.21)]; the content of glutamic acid was (12.3±1.2), (12.0±0.8) , (10.2±0.6), and (11.8 ±1.0) μmol/g in NS control group, DMPS control group, TETS control group, and DMPS protection group, respectively. The OD value of autoradiograms decreased in TETS group compared with buffer control group in cortex, hippocampus, diencephalon, and brain-stem [(0.084 ± 0.008), (0.081 ± 0.009), (0.094 ± 0.006) and (0.081 ± 0.006), vs (0.102 ± 0.003), (0.109 ± 0.005), (0.128 ± 0.007), and (0.125 ± 0.008), respectively]. OD value was maintained orhigher than the normal level in DMPS + TETS group in the four brain areas [(0.116 ± 0.008), (0.125 ± 0.011), (0.129 ± 0.005), and (0.128 ± 0.010) vs (0.102±0.003), (0.109±0.005), (0.128 ± 0.007), and (0.125 ±0.008), respectively]. CONCLUSION: The inhibitory effects of DMPS on the antagonism of TETS to GABA receptor are due to the increase in the GABA binding to its receptors in brain caused by DMPS.目的:探讨二巯丙磺钠(DMPS)对四次甲基二砜四胺(TETS)拮抗GABA受体的影响。方法:通过急性毒性试验观察DMPS和TETS对小鼠的影响;利用氨基酸自动分析仪测定小鼠脑内游离氨基酸的变化;通过宏观放射自显影术观察不同实验组中[~3H]-GABA与其受体结合情况。结果:与NS对照组比较,icv和ip DMPS后小鼠的惊厥数从20只下降至4只和2只;小鼠脑内游离GABA含量与DMPS保护组和生理盐水组比较,DMPS对照组和TETS对照组含量均有变化[μmol/g:(2.09±0.05)和(2.67±0.15),vs(2.40±0.10)和(2.41±0.21)];在NS对照组、DMPS对照组、TETS对照组和DMPS保护组中,小鼠脑内游离的谷氨酸(Glu)含量分别是(12.3±1.2),(12.0±0.8),(10.2±0.6)和(11.8±1.0)μmol/g。与缓冲液对照组大鼠脑片中不同脑区[(0.102±0.003),(0.109±0.005),(0.128±0.007)和(0.125±0.008)]比较,TETS组放射自显影图像中大脑皮质、海马、间脑、脑干的光密度显著降低[(0.084±0.008),(0.081±0.009),(0.094±0.006),和(0.081±0.006)];DMPS+TETS组中不同脑区的光密度[(0.116±0.008),(0.125±0.011),(0.129±0.005)和(0.128±0.010)]维持或高于正常水平[(0.102±0.003),(0.109±0.005),(0.128±0.007)和(0.125±0.008)]。结论:DMPS通过增加脑内GABA与受体的结?

关 键 词：sodium dimercaptopropanesulfonate tetramethylenedisulphotetramine GABA receptors auto- radiography 

分 类 号：R96[医药卫生—药理学]