Comparison of the Anticonvulsant Activities of Substituted Hydroxycoumarins and 4-[(3-Nitro-2-Oxo-2H-Chromen-4-Yl)Amino]Butanoic Acid

被引:0
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作者
E. E. Yakovleva
L. V. Myznikov
P. D. Shabanov
机构
[1] Institute of Experimental Medicine,
[2] Russian Academy of Medical Sciences,undefined
来源
Pharmaceutical Chemistry Journal | 2020年 / 54卷
关键词
coumarin derivatives; anticonvulsant activity; nicotine convulsions; corazole convulsions; mice;
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学科分类号
摘要
The anticonvulsant activity of hydroxycoumarin derivatives and 4-[(3-nitro-2-oxo-2H-chromen-4-yl)amino] butanoic acid was studied using nicotine and corazole convulsion models. All investigated compounds protected animals from death in 100% of cases after intraperitoneal administration of the LD50 of nicotine (14 mg/kg). 4-[(3-Nitro-2-oxo-2H-chromen-4-yl)amino]butanoic acid showed anticonvulsant activity at a dose of 20 mg/kg in the corazole convulsion test while 7-(2-morpholino-2-oxoethoxy)-2H-chromen-2-one (a 7-hydroxycoumarin derivative) prevented convulsions at a dose of 200 mg/kg, which was comparable to the anticonvulsant effect of valproic acid at the same dose. An analysis of the results suggested different mechanisms for the anticonvulsant action of the investigated substances, which was indicative of good prospects for further development of coumarin derivatives as agents with wide spectra of anticonvulsant activity.
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页码:904 / 908
页数:4
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