一种四唑并喹啉化合物的抗惊厥活性研究

Anticonvulsant Activity Evaluation of a Kind of Tetrazolo[1,5-a]quinolone Compound

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.