[Intake dynamics of GABA and its pantoate derivative in mice brain areas].

Ukrains'kyi biokhimichnyi zhurnal Pub Date : 1977-11-01
V A Rozanov, V M Kopelevich, I V Savits'kiĭ, A Ia Rozanov
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Abstract

After subcutaneous administration in equimolar, close to therapeutic, doses accumulation of 1-14C-PANTOGAB exceeds accumulation of 1-14C-GABA in the brain areas only at early stages of observations: 7.5 and 15 min. In blood at all the time except for 4 h, the amount of 1-14C-PANTOGAB exceeds essentially the content of 1-14C-GABA. Maximum of 14C-PANTOGAB accumulation in the brain is observed 30 min later and that of 14C-GABA by 60 min. Difference in distribution of both preparations between the brain areas are inconsiderable. In the period of maximum accumulation there is a tendency to a more intensive 1-14C-PANTOGAB incorporation into the cerebellum, and 1-14C-GABA into truncus cerebri. The dynamics of accumulation in the brain and removing of the studied compounds from blood evidences for better absorption from the place of administration and for a weaker biotransformation of PANTOGAB as compared to GABA.

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[GABA及其泛酸衍生物在小鼠脑区的摄入动态]。
在等量皮下给药后,接近治疗,1-14C-PANTOGAB的剂量积累仅在观察的早期阶段(7.5和15分钟)超过脑区1-14C-GABA的积累。除4小时外,血液中1-14C-PANTOGAB的量基本上超过1-14C-GABA的含量。14C-PANTOGAB在30分钟后达到脑内累积最大值,14C-GABA在60分钟后达到最大值。两种制剂在脑区的分布差异不大。在最大积累期,1-14C-PANTOGAB倾向于更密集地进入小脑,1-14C-GABA倾向于进入脑干。PANTOGAB在大脑中的积累和从血液中去除所研究的化合物的动态表明,与GABA相比,PANTOGAB在给药部位的吸收更好,生物转化更弱。
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