Gordon R, Gels M, Diamantis W, Sofia R D
Wallace Laboratories, Division of Carter-Wallace, Inc., Cranbury, NJ 08512.
Pharmacol Biochem Behav. 1991 Sep;40(1):109-13. doi: 10.1016/0091-3057(91)90329-z.
The anticonvulsant effects of felbamate alone or in combination with diazepam were investigated against maximal electroshock-, pentylenetetrazol-, isoniazid- and bicuculline-induced seizures in mice. A single subprotective dose of felbamate, a dose which offers no protection to animals when combined with diazepam, enhanced the protective effects of diazepam against seizures induced by electroshock, pentylenetetrazol and isoniazid, as measured by significant reduction of ED50 values. However, felbamate failed to significantly affect the protective action of diazepam against bicuculline. Felbamate does not interact directly with the GABA-benzodiazepine-ionophore complex. Thus the enhancement of anticonvulsant activity of diazepam by felbamate against maximal electroshock and pentylenetetrazol may involve an indirect effect at benzodiazepine receptors. The anticonvulsant action of felbamate against isoniazid does not seem to involve benzodiazepine receptors and may be due to reversing the inhibitory effect of isoniazid on glutamate decarboxylase (GAD) activity. The interaction between felbamate and diazepam may also involve other mechanisms.
研究了非氨酯单独或与地西泮联合使用对小鼠最大电休克、戊四氮、异烟肼和荷包牡丹碱诱导惊厥的抗惊厥作用。非氨酯的单一亚保护剂量(与地西泮联合使用时对动物无保护作用的剂量)增强了地西泮对电休克、戊四氮和异烟肼诱导惊厥的保护作用,通过显著降低半数有效剂量(ED50)值来衡量。然而,非氨酯未能显著影响地西泮对荷包牡丹碱的保护作用。非氨酯不直接与γ-氨基丁酸-苯二氮䓬-离子载体复合物相互作用。因此,非氨酯增强地西泮对最大电休克和戊四氮的抗惊厥活性可能涉及对苯二氮䓬受体的间接作用。非氨酯对异烟肼的抗惊厥作用似乎不涉及苯二氮䓬受体,可能是由于逆转了异烟肼对谷氨酸脱羧酶(GAD)活性的抑制作用。非氨酯与地西泮之间的相互作用也可能涉及其他机制。