Antiepileptic drugs have a number of mechanisms of action that target brain excitability systems. The potentiation of GABAergic inhibitory neurotransmission represents a classic and well-known antiseizure effect. Currently available GABAergic antiepileptic drugs mainly target GABA(A) receptor-associated complexes, GABA reuptake or GABA catabolism. All these compounds, although generally effective, are limited by their deleterious effects on cognition and behavior. The challenge will be to find GABAergic drugs that exhibit the beneficial effects, without the adverse ones.
[Show abstract][Hide abstract] ABSTRACT: alpha-asarone is a major essential oil component of rhizomes of Acori Graminei Rhizoma (AGR), a traditional medicinal plant utilized in China to treat epilepsy. The objective of present study was to investigate the antiepileptic activity of alpha-asarone in various animal seizure models. Experimental seizure models were established in mice and rats in which the antiepileptic properties of alpha-asarone were compared with those of Valproic Acid (VPA), Carbamazepine (CBZ) and Clonazepam (CNP). The Maximal Electroshock Seizure (MES) test and Subcutaneous Pentylenetetrazol Seizure (scPTZ) test were done in Kunming (KM) mice. The lithium-pilocarpine model was employed to assess the antiepileptic activity in rats. The seizure incidence significantly decreased by 40-100% in the MES test, 50-90% in the scPTZ test and 40-80% in the lithium-pilocarpine model; the seizure latency dramatically prolonged by 180 sec in the scPTZ test and 4-15 min in the lithium-pilocarpine model; the seizure severity score was markedly reduced by 1.96 in the lithium-pilocarpine model. The seizure frequency markedly reduced in the lithium pilocarpine model. In addition, significant differences in the above variables were noted between alpha-asarone at 200 mg kg(-1) (p.o.) and that at 50 or 100 mg kg(-1). These results suggest that alpha-asarone has favorable antiepileptic activity, is an active antiepileptic drug and has potential implication in the management of epilepsy.
International Journal of Pharmacology 06/2012; 8(6):567-571. DOI:10.3923/ijp.2012.567.571 · 0.71 Impact Factor
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