长期的影响与阿尔法2-adrenoceptor拮抗剂米氮平治疗5 -神经传递。

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Haddjeri N,布莱P, de Montigny C

长期的影响与阿尔法2-adrenoceptor拮抗剂米氮平治疗5 -神经传递。

Naunyn Schmiedebergs拱杂志。1997年1月,355 (1):20-9。

PubMed ID

9007838 (在PubMed

]

文摘

米氮平(ORG 3770, Remeron)是一种非选择性α2-adrenoceptor拮抗剂在抑郁症与抗抑郁药活动。本研究的目的是评估,使用一个体内电生理学的范式,长期治疗的效果与米氮平预处理和突触后α2-adrenoceptors和5 -神经传递男性Sprague-Dawley老鼠。一个21天的米氮平治疗(5毫克/公斤/天,南卡罗来纳州。,使用渗透微型泵)蓝斑的自发放电活动增加去甲肾上腺素(NA)神经元。他们的发射活动恢复正常后48 h移除微型泵。然而,这种治疗没有修改的抑制效应的剂量反应曲线α2-adrenoceptor受体激动剂氯压定NA神经元的放电活动。中缝背5 -神经元的自发放电活动在mirtazapine-treated老鼠也显著增加,并恢复正常后48 h微型泵的移除。可乐定的抑制效应的剂量反应曲线5 -神经元的放电活动在mirtazapine-treated改变了老鼠。此外,它进一步转移到左边后48小时惨败。米氮平治疗长期不修改microiontophoretically-applied NA的抑制效应和5 - CA3背侧海马锥体神经元的放电活动。 However, this mirtazapine treatment antagonized both the enhancing effect of a low dose (10 micrograms/kg, i.v.) and the reducing effect of a high dose (100 micrograms/kg, i.v.) of the alpha 2-adrenoceptor agonist clonidine on the effectiveness of the electrical stimulation of the ascending 5-HT pathway in suppressing the firing activity of dorsal hippocampus CA3 pyramidal neurons. After a 48-h washout, only the effect of the high dose of clonidine was attenuated, suggesting a desensitization of the terminal alpha 2-adrenergic heteroreceptor, but not of the terminal alpha 2-adrenergic autoreceptor. The decrease in the effectiveness of the stimulation upon increasing its frequency from 1 to 5 Hz (due to the activation of terminal 5-HT autoreceptors) was unaltered after the long-term mirtazapine treatment. In conclusion, the tonic activation of postsynaptic 5-HT receptor is enhanced by a 21-day treatment with mirtazapine, as a result of a sustained increase in 5-HT neuron firing activity in the presence of decreased function of alpha 2-adrenergic heteroreceptors located on 5-HT terminals in the dorsal hippocampus.

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药物靶点

药物	目标	类	生物	药理作用	行动
米氮平	Alpha-2A肾上腺素能受体	蛋白质	人类	是的	拮抗剂	细节