Getova D, Georgiev V
Experimental Pharmacology Department, Bulgarian Academy of Sciences.
Acta Physiol Pharmacol Bulg. 1988;14(2):49-55.
The effect of the newly synthesized barbiturate HB-7 (2-hydroxylamino-5-ethyl-5-sec. pentylbarbituric acid) was investigated in experiments on mice in comparison with the effect of pentobarbital (PB), as well as their correlations with agents potentiating GABA-ergic transmission: GABA, aminooxyacetic acid, nipecotic acid, di-n-propylacetate (depakin, DPA), muscimol and baclofen. After the test applied (electroshock convulsions) 50 per cent of the animals in the control group had a tonic convulsion. HB-7 and all the other agents were administered in threshold doses. GABA-ergic agents were found to have a different effect on the anticonvulsive action of HB-7 and of pentobarbital. The anticonvulsive effect of HB-7 was potentiated when it was applied in combination with baclofen and AOAA, and partially with depakin (DPA). The anticonvulsive action of pentobarbital is potentiated when it is administered in combination with DPA and AOAA. The results obtained suggest that the GABA-ergic transmission in the brain participates in the anticonvulsive effects of the barbiturates investigated (HB-7 and PB).
在小鼠实验中，研究了新合成的巴比妥酸盐HB - 7（2 - 羟基氨基 - 5 - 乙基 - 5 - 仲戊基巴比妥酸）的作用，并与戊巴比妥（PB）的作用进行了比较，以及它们与增强GABA能传递的药物之间的相关性：GABA、氨氧基乙酸、哌啶酸、二正丙基乙酸（丙戊酸，DPA）、蝇蕈醇和巴氯芬。在应用测试（电击惊厥）后，对照组中有50%的动物出现强直性惊厥。HB - 7和所有其他药物均以阈剂量给药。发现GABA能药物对HB - 7和戊巴比妥的抗惊厥作用有不同影响。当HB - 7与巴氯芬和氨氧基乙酸联合应用时，其抗惊厥作用增强，与丙戊酸（DPA）联合应用时部分增强。戊巴比妥与丙戊酸和氨氧基乙酸联合应用时，其抗惊厥作用增强。所得结果表明，大脑中的GABA能传递参与了所研究的巴比妥酸盐（HB - 7和PB）的抗惊厥作用。
