Saano V
Med Biol. 1986;64(4):201-6.
The effect of tofizopam, a 3,4-benzodiazepine (BZ) derivative, in modulating the anticonvulsive action of various drugs was investigated in mice. Electric shock and intravenous infusion of bicuculline were used as convulsive agents. Tofizopam increased the action of clonazepam, diazepam and flunitrazepam against bicuculline. The anticonvulsive effect of diazepam against electroshocks was augmented only slightly. Tofizopam failed to alter the actions of carbamazepine, phenobarbital, phenytoin, or sodium valproate against either of the convulsive stimuli. Both in vitro and in vivo, tofizopam has been shown to stimulate the binding of 1,4-BZs (e.g., flunitrazepam) to BZ receptors. Similarly, tofizopam enhances the binding of muscimol to GABA receptors. Although several anticonvulsants act on the GABA-BZ receptor complex, tofizopam seems to modify selectively the anticonvulsive action of 1,4-BZs, and this effect is seen better in bicuculline-induced seizures than in electroshocks.
在小鼠中研究了3,4 -苯二氮䓬（BZ）衍生物托非佐泮在调节各种药物抗惊厥作用方面的效果。电击和静脉注射荷包牡丹碱用作惊厥剂。托非佐泮增强了氯硝西泮、地西泮和氟硝西泮对荷包牡丹碱的作用。地西泮对电击的抗惊厥作用仅略有增强。托非佐泮未能改变卡马西平、苯巴比妥、苯妥英或丙戊酸钠对任何一种惊厥刺激的作用。在体外和体内，托非佐泮均已显示能刺激1,4 - BZs（如氟硝西泮）与BZ受体的结合。同样，托非佐泮增强了蝇蕈醇与GABA受体的结合。尽管几种抗惊厥药作用于GABA - BZ受体复合物，但托非佐泮似乎选择性地改变1,4 - BZs的抗惊厥作用，并且这种作用在荷包牡丹碱诱导的惊厥中比在电击惊厥中更明显。
