Since a previous study indicated that the water extract of Scutellariae rad
ix (SR) had high affinity for the benzodiazepine (BDZ) binding site of GABA
(A), receptors, the present study examined whether SR water extract has an
anticonvulsant effect in vivo and an enhancing effect on gamma -amino-n-but
yric acid (GABA)-stimulated uptake of Cl-36(-) in cortex preparation in vit
ro in mice. The results showed that SR water extract had little effect on p
entylenetetrazol (PTZ, 85 mg/kg, s.c.)-induced clonic seizures but signific
antly inhibited maximal electroshock-induced tonic seizures with an ED50 of
3.6 g/kg. The BDZ agonist chlordiazepoxide (10 mg/kg, i.p.) had anticonvul
sant activity on both types of seizures. In Cl-36(-) uptake assay, SR water
extract (1-500 mug/ml) had no significant effect on 25 muM GABA-stimulated
Cl-36(-) uptake, whereas chlordiazepoxide (10 muM) increased the Cl-36(-)
uptake to 125% of control. Therefore, the present results showed for the fi
rst time that SR water extract had anticonvulsant activity against maximal
electroshock-induced tonic seizures, and suggested that this anticonvulsant
effect might be not via the activation of the BDZ binding site of GABA(A)
receptors, but probably via the prevention of seizure spread. (C) 2000 Else
vier Science Ireland Ltd. All rights reserved.