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Background: Diketones and α,β-unsaturated ketone are useful intermediates for the synthesis of antiepileptic moieties. Epilepsy is a neurological disorder that affects about fififty million people worldwide. The aim of the study was to assess benzylideneacetophenone analogues for their potential antiepileptic effects in mice.
Methods: The compounds used in the pharmacological assay which include; 4-Dimethylaminochalcone (A), 1(4-Nitrophenyl) – 3 (ϒ -benzopyranoyl)-2-propen – 1-one (B), 1(4' –Nitrophenyl) – 3 (1,3-benzodioxolyl) 2 – propen – 1 – one (C), 1-Phenyl-3- (benzodioxolyl) – 2 –propen – 1-one (D), 4-Chlorochalcone (E), 4'-Nitro-4-dimethylaminochalcone (F) 4'-Nitro-4-methoxychalcone (G), were assayed using three models; Strychnine, Pentylenetetrazole (PTZ) and Maximal Electroshock (MES). The samples were given at 500, 1000 and 1500 mg/kg while standard drug diazepam and distilled water were given at 5 mg and 10 ml/kg intraperitoneal respectively. Convulsion inducing agents (Strychnine 2 mg/kg and PTZ, 100 mg/kg) were administered intraperitoneal 1hour after the administration of test samples while MES model electroconvulsive shock was applied using electroconvulsive machine.
Results: The samples (A-G) showed significant (P<0.03, 0.003, 0.0007 and 0.0001) effect in delaying onset of seizure compared to control in strychnine model, while in PTZ model samples (A-F) evaluated at 500,1000 and 1500 mg/kg are equipotent at all the doses by signifificantly (P<0.0001) and sample G (P<0.0007) reduced the onset of seizure compared to control. However in MES model samples (A-F and G) evaluated at 500, 1000 and 1500 mg/kg are equipotent at all the doses by significantly (P<0.0001; 0.0007), reduced the duration of seizure compared to control respectively.
Conclusion: Benzylideneacetophenone analogues showed various effects in control of seizure in all the models used.This effect is due to delayed onset and reduction of seizure duration. The samples could act by stimulating the glycine, Gamma Aminobutyric acid (GABA) receptor, inhibition of GABAAminotransferase and prolong inactivation of sodium ion channel.
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