1347727-71-2Relevant academic research and scientific papers
Synthesis and anticonvulsant activity of trans- and cis-2-(2,6- dimethylphenoxy)-N-(2- or 4-hydroxycyclohexyl)acetamides and their amine analogs
Pkala, Elbieta,Waszkielewicz, Anna M.,Szneler, Edward,Walczak, Maria,Marona, Henryk
, p. 6927 - 6934 (2012/01/06)
A group of trans- and cis-2-(2,6-dimethylphenoxy)-N-(2-hydroxycyclohexyl) acetamides (1-7) and -ethylamines (8-9) have been synthesized and investigated for their anticonvulsant activity. One of them, racemic trans-2-(2,6- dimethylphenoxy)-N-(2-hydroxycyclohexyl)acetamide proved to be the most effective in MES (mice, ip), exhibiting ED50 = 42.97 mg/kg b.w. and TD50 = 105.67 mg/kg b.w. It also proved protection in focal seizures (electric kindling, rats, ip) and it raises seizure threshold. The mechanism of action is inhibition of voltage-gated sodium currents and enhancement of GABA effect. Safety pharmacology assay on threshold tonic extension revealed no lowering of the seizure threshold.
