Getova D, Markovska V
Experimental Pharmacology Department, Bulgarian Academy of Sciences.
Acta Physiol Pharmacol Bulg. 1988;14(2):56-62.
The effects of two newly synthesized barbiturates--HB-7 (2-hydroxylamino-5-ethyl-5-sec. pentylbarbituric acid) and HB-2 (2-hydroxylamino-5-ethyl-5-propylbarbituric acid--on models of apomorphine stereotypy and haloperidol catalepsy were investigated in experiments on male rats and mice. The test drugs used were phenobarbital (PB)--in stereotypy and catalepsy, and diphenylhydantoin (DPH)--in catalepsy. HB-7 changes the stereotypy considerably: it developed faster and disappeared faster than in the control group. Phenobarbital had a weaker effect on the intensity and duration of the stereotypy. Catalepsy was induced with haloperidol in doses of 1 and 2 mg/kg. HB-7 and HB-2 weakened haloperidol catalepsy, compared with PB and DPH. The faster occurrence of apomorphine stereotypy and the weakening of the haloperidol-induced catalepsy under the effect of the two hydroxyl-amine derivatives of barbituric acid suggest an effect on the cerebral dopaminergic transmission. This effect may be mediated through the effect of HB-7 on DA-ergic transmission or through the GABA-ergic transmission in the brain structures responsible for these behavioural reactions.
在雄性大鼠和小鼠实验中,研究了两种新合成的巴比妥酸盐——HB - 7(2 - 羟氨基 - 5 - 乙基 - 5 - 仲戊基巴比妥酸)和HB - 2(2 - 羟氨基 - 5 - 乙基 - 5 - 丙基巴比妥酸)对阿扑吗啡刻板行为模型和氟哌啶醇僵住症模型的影响。所使用的对照药物为苯巴比妥(PB)——用于刻板行为和僵住症实验,以及苯妥英钠(DPH)——用于僵住症实验。HB - 7对刻板行为有显著影响:与对照组相比,其出现更快且消失也更快。苯巴比妥对刻板行为的强度和持续时间影响较弱。用1和2mg/kg剂量的氟哌啶醇诱导僵住症。与PB和DPH相比,HB - 7和HB - 2可减弱氟哌啶醇诱导的僵住症。巴比妥酸的两种羟胺衍生物作用下阿扑吗啡刻板行为更快出现以及氟哌啶醇诱导的僵住症减弱,提示其对脑多巴胺能传递有影响。这种影响可能是通过HB - 7对多巴胺能传递的作用,或通过在负责这些行为反应的脑结构中的γ - 氨基丁酸能传递介导的。