Anticonvulsant activity of piperine on seizures induced by excitatory amino acid receptor agonists.

In traditional Chinese medicine, a mixture of radish and pepper is used to treat epilepsy. The presumptive effectiveness of this prescription might be due to the anticonvulsant actions of the principal component of pepper, the alkaloid piperine (CAS 94-62-2). The effects of piperine on convulsions induced in mice by agonists at different excitatory amino acid receptor subtypes were studied. Piperine was shown to significantly block convulsions induced by intracerebroventricular injection of threshold doses of kainate, but to have no or only slight effects on convulsions induced by L-glutamate, N-methyl-D-aspartate or guanidinosuccinate. Piperine suspensions, injected intraperitoneally, 1 h before injection of the threshold intracerebroventricular dose of kainate for the induction of clonic convulsions (1 nmol), blocked these convulsions with an ED50 (and 95% confidence interval) of 46 (25-86) mg/kg. Although piperine did block convulsions, induced by kainate, the compound does not appear to act as a kainate receptor antagonist. Whole-cell currents induced by the application of kainate to spinal cord cells in primary dissociated cultures were not affected by co-application of piperine.