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Article Abstract
To discover novel, potent anticonvulsant compounds, a series of compounds containing triazole structural fragments were synthesized and evaluated for their anticonvulsant activity. Compounds (maximal electroshock (MES), 50% effective dose (ED) = 13.1 mg/kg; subcutaneous pentylenetetrazole (scPTZ), ED = 19.7 mg/kg) and (MES, ED = 9.1 mg/kg; PTZ, ED = 19.0 mg/kg) showed the best activity in MES and PTZ tests. The results of an affinity test showed that the potent compounds had better binding to the GABA receptors. The results of an inhibitory neurotransmitter GABA content test in brain tissue indicated that compounds and exerted anticonvulsant activity which may be associated with the increase of GABA content in the rat brain. Elevated plus maze (EPM) assay results showed that compounds and possessed anxiolytic effects, and their effects correlated with the binding sites of benzodiazepines (BZs) in the GABA receptors. Molecular docking was performed to investigate the interactions of the studied compound with the GABA receptors on the molecular level.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC12388125 | PMC |
| http://dx.doi.org/10.3390/molecules30163400 | DOI Listing |
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