摘要
为了评价4,5-二氢-7-(4-氯苯氧基)-四唑[1,5-a]喹啉(S2011017)的抗癫痫活性,采用最大电惊厥(Maximum Electron Shock,MES)实验、多种化学致惊实验及急性神经毒性实验,测定了其作用时间和剂量关系。MES实验结果表明,腹腔给药5 min后,S2011017表现出较好的抗癫痫活性(ED50=11.8 mg·kg-1)。在化学致惊实验中,S2011017对异烟肼(ISO),3-巯基丙酸(3-MP),荷包牡丹碱(BIC)和硫代氨基脲(THIO)引起的惊厥有效。因此,由于S2011017表现出广谱的抗惊厥活性,并且能够快速地达到抗惊厥活性的峰值,可以作为一种潜在抗癫痫药,进行深入的成药性评价。
An anticonvulsant characterized of 7- (4-chlorobenzyloxy) -4, 5-dihydrotetrazolo [1, 5-a] quinoline (S2011017)wasevaluated the relationship between its dose and action time by numerous experimental seizure models, containing maximalelectroshock(MES) -, pentylenetetrazole(PTZ) -,isoniazid(ISO) -, 3-mercaptopropionic acid(3-MP) -, bicucullin (BIC) -,thiosemicarbazide (THIO) -,and strychnine(STR) -induced seizures.The result of MES showed that 5 min after its intraperitoneal(i.p.)administration, S2011017 gave better anticonvulsant activity (ED50=11.8 mg· kg -1) . In several chemical compounds inducedseizures experiments,S2011017 had the anticonvulsant activity effect on ISO,3-MP, BIC and THIO. Based on this study, the anti-depression compound S2011017 was concluded to have anticonvulsant activity and reach peak value, so it would be worthy of furtherpharmacological test.
作者
荆博涛
刘媚钰
钟春艳
孙先宇
Jing Botao;Liu Meiyu;Zhong Chunyan;Sun Xianyu(College of Animal Science and Technology,Heilongjiang Bayi Agricultural University,Daqing 163319)
出处
《黑龙江八一农垦大学学报》
2018年第5期46-49,共4页
journal of heilongjiang bayi agricultural university
基金
特异性COX-2抑制剂的设计
合成及筛选(黑龙江省青年科学基金项目QC2014C106)
黑龙江省普通高等学校青年学术骨干支持计划(1252G041)