Wahlström G, Norberg L
Brain Res. 1984 Sep 24;310(2):261-7. doi: 10.1016/0006-8993(84)90149-5.
The sensitivities in the brain of the barbiturates N-methyl-cyclobarbital (MCB) and hexobarbital (HEX) were determined by an anesthesia threshold in male rats. The criterion was a burst suppression in the EEG of 1 s or more (the 'silent second'). The dose needed to induce the criterion was used as the threshold. Available for testing were with MCB the isomers and the racemate and with HEX the isomers and various combinations of them. In experiment 1 the 4 isomers and the racemates were all tested in the same group of animals. In experiment 2 various combinations of HEX were tested. With HEX the (+)-S-isomer and with MCB the (-)-R-isomer was the most potent one. The differences in anesthetic action between the isomers were largest with HEX. During induction of anesthesia no jerks were recorded with (-)-R-MCB. All the other isomers induced jerks. The only significant regression found, when all isomers were tested against each other, was a negative one between (-)-R-MCB and (-)-R-HEX (r = -0.79). No significant relations were found between the isomers and the corresponding racemate. Experiments with the racemate of MCB and with various combinations of the isomers of HEX indicated that a potentiation appeared when the isomers were used together.
通过雄性大鼠的麻醉阈值来确定巴比妥类药物N-甲基环巴比妥(MCB)和己巴比妥(HEX)在大脑中的敏感性。判断标准是脑电图中出现持续1秒或更长时间的爆发抑制(“沉默秒”)。诱导达到该标准所需的剂量用作阈值。可用于测试的,对于MCB有异构体和外消旋体,对于HEX有异构体及其各种组合。在实验1中,4种异构体和外消旋体都在同一组动物中进行了测试。在实验2中,测试了HEX的各种组合。对于HEX,(+)-S-异构体最有效,对于MCB,(-)-R-异构体最有效。异构体之间麻醉作用的差异在HEX中最大。在麻醉诱导期间,(-)-R-MCB未记录到抽搐。所有其他异构体均诱导出抽搐。当所有异构体相互测试时,唯一发现的显著回归是(-)-R-MCB和(-)-R-HEX之间的负相关(r = -0.79)。异构体与相应外消旋体之间未发现显著关系。用MCB的外消旋体和HEX异构体的各种组合进行的实验表明,异构体一起使用时会出现增效作用。