藁苯内酯对GABA_A受体的激动作用
Effect of Z-ligustilide on GABA_A receptor in vitro and in vivo
作者：王宇;赖鹏;李永杰;杜俊蓉;
Author：
收稿日期： 年卷（期）页码：2014,29(02):-152-154
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：藁苯内酯(LIG);GABAA受体;神经保护
Key words：
基金项目：国家自然科学基金资助项目(批准号:81072636)
中文摘要
目的研究藁苯内酯(LIG)在体内外对GABAA受体的作用。方法体外实验中,用3H氟硝西泮作为放射性标记物,用放射性配体受体结合实验测定LIG对GABAA受体的结合能力;体内实验中,以皮下注射戊四唑90 mg·kg-1致小鼠惊厥为病理模型,用LIG(20、40 mg·kg-1)或地西泮(10 mg·kg-1)提前30 min于腹腔给药进行干预,60 min内观察动物的行为。结果 LIG对GABAA受体的苯二氮类结合位点有较高的亲和力,IC50为170 nmol·L-1;LIG能明显延长惊厥发生的潜伏期(P
参考文献
[1]Zorumski CF,Isenberg KE.Insights into the structure and function of GABA-benzodiazepine receptors:Ion channels and psychiatry[J].Am J Psychiatry,1991,148(2):162-173.
[2]Frolund B,Ebert B,Kristiansen U,et al.GABAAreceptor ligands and their therapeutic potentials[J].Curr Top Med Chem,2002,2(16):817-832.
[3]Lanctt KL,Herrmann N,Mazzotta P,et al.GABAergic function in Alzheimer’s disease:Evidence for dysfunction and potential as a therapeutic target for the treatment of behavioural and psychological symptoms of dementia[J].Can J Psychiatry,2004,49(7):439-453.
[4]Ricci L,Valoti M,Sgaragli G,et al.Neuroprotection afforded by GABA against oxygen-glucose deprivation induced injury in rat cortical brain slices:Anhormetic dose-response effect[J].Am J Pharmacol Toxicol,2008,3(1):160-167.
[5]Kuang X,Du JR,Chen YS,et al.Protective effect of Z-ligustilide against amyloid beta-induced neurotoxicity is associated with decreased pro-inflammatory markers in rat brains[J].Pharmacol Biochem Behav,2009,92(4):635-641.
[6]Chen SW,Min L,Li WJ,et al.The effects of angelica essential oil in three murine tests of anxiety[J].Pharmacol Biochem Behav,2004,79(2):377-382.
[7]Deng S,Chen SN,Lu J,et al.GABAergic phthalide dimmers from Angelica sinesis(Oliv.)Diels[J].Phytochem Anal,2006,17(6):398-405.
[8]Ricci L,Valoti M,Sgaragli G,et al.Neuroprotection afforded by diazepam against oxygen/glucose deprivation-induced injury in rat cortical brain slices[J].Eur J Pharmacol,2007,561(1-3):80-84.
【关闭】
