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丙戊酸钠:大鼠不同脑区的药代动力学特征及其对γ-氨基丁酸水平的影响。

Sodium valproate: kinetic profile and effects on GABA levels in various brain areas of the rat.

作者信息

Mesdjian E, Ciesielski L, Valli M, Bruguerolle B, Jadot G, Bouyard P, Mandel P

出版信息

Prog Neuropsychopharmacol Biol Psychiatry. 1982;6(3):223-33. doi: 10.1016/s0278-5846(82)80172-3.

Abstract
  1. The kinetic profile of sodium valproate (VPA) and the GABA levels were studied in discrete brain areas of the rat after an i.p. injection of 200 mg/kg. The results were discussed comparatively with GABA-T and GAD activities reported in the literature. 2. VPA was rapidly distributed in brain areas; its concentrations, its kinetic parameters and the GABA levels after the drug administration were not uniform in the different brain areas studied. 3. The results showed a particular relation of the VPA to the olfactory bulbs; in this specific area the VPA effect on GABA level was stronger; the VPA apparent half life of elimination was longest; the VPA apparent disappearance rate constant was smallest; the initial GABA level was higher; the activities of GABA-T and GAD were higher than in other brain areas studied except the hypothalamus. 4. These data were correlated with the role of the olfactory bulbs in the behaviour of the rodents.
摘要
  1. 腹腔注射200mg/kg丙戊酸钠(VPA)后,研究了大鼠离散脑区中丙戊酸钠的动力学特征及γ-氨基丁酸(GABA)水平。将结果与文献报道的GABA转氨酶(GABA-T)和谷氨酸脱羧酶(GAD)活性进行了比较讨论。2. VPA在脑区中分布迅速;给药后其浓度、动力学参数及GABA水平在不同研究脑区中并不一致。3. 结果显示VPA与嗅球存在特定关系;在这个特定区域,VPA对GABA水平的影响更强;VPA的表观消除半衰期最长;VPA的表观消失速率常数最小;初始GABA水平较高;GABA-T和GAD的活性高于除下丘脑外的其他研究脑区。4. 这些数据与嗅球在啮齿动物行为中的作用相关。

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