Duka T, Wüster M, Herz A
Naunyn Schmiedebergs Arch Pharmacol. 1979 Oct;309(1):1-5. doi: 10.1007/BF00498749.
The acute treatment of rats with diazepam induces pronounced changes in brain enkephalin concentrations, as was estimated for methionine(met)-enkephalin and in some representative experiments for leucine(leu)-enkephalin, employing highly specific radioimmunoassays. Diazepam selectively increased the enkephalin concentrations in the hypothalamus by about 35%, and lowered it in the corpus striatum by roughly 25%; no changes could be detected in the medulla oblongata/pons or midbrain. The drug-induced changes displayed a rapid onset. Peak effects were reached by 2 to 5 min after injection. Changes observed in the hypothalamus were only short lasting and were apparently parallelled by diazepam concentrations in the brain, whereas the decrease in the striatum was of markedly longer duration. Presently, the mechanism underlying all these changes is unknown. Whereas an increase in enkephalin concentrations in the hypothalamus may be discussed in terms of the anti-stress effect of benzodiazepines, the observed drop in striatal enkephalin is not obviously to be correlated to behavioural changes induced by these drugs.
用安定对大鼠进行急性处理会引起脑内脑啡肽浓度的显著变化,这是通过高特异性放射免疫测定法对甲硫氨酸(met)-脑啡肽进行估算得出的,在一些代表性实验中对亮氨酸(leu)-脑啡肽也进行了测定。安定选择性地使下丘脑内的脑啡肽浓度增加约35%,而使纹状体内的脑啡肽浓度降低约25%;在延髓/脑桥或中脑未检测到变化。药物诱导的变化起效迅速。注射后2至5分钟达到峰值效应。下丘脑观察到的变化只是短暂的,且显然与脑内安定浓度平行,而纹状体中的降低持续时间明显更长。目前,所有这些变化背后的机制尚不清楚。虽然下丘脑内脑啡肽浓度的增加可以从苯二氮䓬类药物的抗应激作用方面进行讨论,但观察到的纹状体脑啡肽下降与这些药物诱导的行为变化并无明显关联。