药物在脑部的摄取。II. 巴比妥酸盐摄取在体外改变氨基酸的转运(1)

Drug uptake by brain. II. Barbiturate uptake alters the transport of amino acids in vitro(1).

Teller D N, De Guzman T, Lajtha A

Vopr Biokhim Mozga. 1974;9:25-41.

Abstract

Valine and leucine uptake into mouse brain slices was stimulated by 1 to 4 mM phenobarbital and pentobarbital. Greater concentrations of these two barbiturates inhibited the transport of these amino acids. Barbital, isobarbituric acid, and 5-nitrobarbituric acid had no effect, while amobarbital and secobarbital produced only inhibition of uptake. 2. Transport of glutamate and aspartate was unaffected by phenobarbital concentrations that inhibited uptake of lysine and alpha-aminoisobutyric acid. 3. Changes in the Na+ and K+ content of the slices were not related to stimulation of valine or leucine uptake. 4. There was no concentrative uptake of phenobarbital by brain slices. The partially saturable uptake of pentobarbital was not by active transport, because the uptake increased after heating brain, liver, or kidney slices to 95 degrees for 10 min. 5. This study shows that individual members of a pharmacologically related group may have specific effects on a composite physiological function (amino acid transport) of brain tissue.

摘要

1至4毫摩尔的苯巴比妥和戊巴比妥可刺激缬氨酸和亮氨酸进入小鼠脑片。这两种巴比妥酸盐的浓度更高时会抑制这些氨基酸的转运。巴比妥、异巴比妥酸和5-硝基巴比妥酸没有影响，而异戊巴比妥和司可巴比妥仅产生摄取抑制作用。2. 抑制赖氨酸和α-氨基异丁酸摄取的苯巴比妥浓度对谷氨酸和天冬氨酸的转运没有影响。3. 脑片的钠和钾含量变化与缬氨酸或亮氨酸摄取的刺激无关。4. 脑片对苯巴比妥没有浓缩摄取。戊巴比妥的部分可饱和摄取不是通过主动转运，因为将脑、肝或肾片加热至95度10分钟后摄取增加。5. 本研究表明，药理相关组中的个别成员可能对脑组织的复合生理功能（氨基酸转运）有特定影响。