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首页> 外文期刊>Neurochemistry International: The International Journal for the Rapid Publication of Critical Reviews, Preliminary and Original Research Communications in Neurochemistry >Interaction between (3H)flunitrazepam and (3H)GABA binding in the cerebellum of reeler mice.
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Interaction between (3H)flunitrazepam and (3H)GABA binding in the cerebellum of reeler mice.

机译：（3H）氟硝西m和（3H）GABA结合在小腹小鼠小脑中的相互作用。

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摘要

It has been shown that in the cerebellum of reeler mutant mice GABA levels and GABA uptake increase while GABA binding decreases. This study shows that in the cerebellum of these mutants there is also an increase of benzodiazepine receptors. This increase is observed in cerebellar homogenates, in nuclei and in membranes. The increase in the density of central (i.e. clonazepam displacable) benzodiazepine receptors is primarily reflected in binding sites located in the GABA-receptor complex. In comparison to wild-type, GABA-modulin extracted from reeler cerebellum inhibits with a greater potency [3H]GABA binding. The increase in the central-type of benzodiazepine binding and its interaction with GABA binding, observed in cerebellar membranes, is interpreted as a functional response to the decrease in GABA binding and may reflect benzodiazepine receptor condensation and/or changes of subunit composition of the GABA/benzodiazepine receptor complex. The enhanced activity of reeler GABA-modulin reflects a functional response to the increased GABA levels in reeler cerebellum. The increase of the peripheral-type (i.e. PK 11195 displacable) of benzodiazepine receptors is probably due to metabolic changes that may accompany reeler cerebellar mutation. Differences in nuclear benzodiazepine binding between reeler and wild-type mice add a physiological importance to the nuclear binding of this drug.
机译：已经表明，在reeler突变小鼠的小脑中，GABA水平和GABA摄取增加，而GABA结合减少。这项研究表明，在这些突变体的小脑中，苯并二氮杂receptor受体也有所增加。在小脑匀浆，细胞核和膜中观察到这种增加。中央（即，氯硝西am可置换）苯并二氮杂receptor受体的密度增加主要反映在位于GABA-受体复合物中的结合位点上。与野生型相比，从re小脑中提取的GABA-调节蛋白具有更强的[3H] GABA结合力。在小脑膜中观察到，苯并二氮杂binding结合的中心类型的增加及其与GABA结合的相互作用被解释为对GABA结合减少的功能性反应，并且可能反映了苯二氮卓受体的缩合和/或GABA亚基组成的变化/苯二氮杂receptor受体复合物。转盘GABA调节蛋白的活性增强反映了对转盘小脑中GABA水平升高的功能性反应。苯二氮卓类受体的外周型（即PK 11195可置换）的增加可能是由于代谢变化引起的，而代谢变化可能伴随着小脑干小脑突变。绕线型小鼠和野生型小鼠之间核仁苯并二氮杂binding结合的差异为该药物的核仁结合增加了生理学重要性。

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