可乐定的作用机制：对单个中枢神经元的影响
On the mechanism of action of clonidine: effects on single central neurones.
作者信息
Anderson C, Stone T W
出版信息
Br J Pharmacol. 1974 Jul;51(3):359-65. doi: 10.1111/j.1476-5381.1974.tb10670.x.
Abstract
1 Noradrenaline and clonidine were applied by microiontophoresis to single neurones in the cerebral cortex and medullary reticular formation of anaesthetized rats.2 Of a total of 247 neurones studied, 79% of medullary units and 60% of cortical units responded in the same manner to both noradrenaline and clonidine. The usual response was a depression of neuronal firing rate.3 It proved possible to antagonize some responses to both substances by the microiontophoresis of bulbocapnine, whilst leaving unaffected similar responses to 5-hydroxytryptamine.4 On 13% of the cells, clonidine produced an increase of firing rate. This effect could not be attributed to a post-synaptic antagonism of tonically released endogenous noradrenaline, but may indicate a presynaptic action of clonidine, reducing noradrenaline release.5 These observations are thought to support the idea that clonidine may have an agonist action on noradrenaline receptors in the brain.
摘要
用微离子透入法将去甲肾上腺素和可乐定施加于麻醉大鼠大脑皮层和延髓网状结构的单个神经元。
在总共研究的247个神经元中，79%的延髓神经元和60%的皮层神经元对去甲肾上腺素和可乐定的反应方式相同。通常的反应是神经元放电频率降低。
事实证明，通过微离子透入法施加荷包牡丹碱可以拮抗对这两种物质的一些反应，而对5-羟色胺的类似反应则不受影响。
在13%的细胞上，可乐定使放电频率增加。这种效应不能归因于对持续释放的内源性去甲肾上腺素的突触后拮抗作用，而可能表明可乐定有突触前作用，减少去甲肾上腺素的释放。
这些观察结果被认为支持这样一种观点，即可乐定可能对大脑中的去甲肾上腺素受体有激动作用。
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