Scuvée-Moreau J J, Dresse A E
Eur J Pharmacol. 1979 Aug 1;57(2-3):219-25. doi: 10.1016/0014-2999(79)90368-6.
The spontaneous firing rate of the noradrenergic neurons of the locus coeruleus and of the serotonergic neurons of the dorsal raphe was recorded with extracellular microelectrodes in chloral hydrate-anesthetized rats. A quantitative comparison of the effect of five tricyclic antidepressants, of tranylcypromine and of mianserin on the spontaneous activity of these two types of cells was performed. All drugs tested, except mianserin reduced the frequency of discharge of the noradrenergic neurons. Intravenous perfusion of the drugs allowed the doses required for inhibition of firing to 50% of the baseline rate (ID50) to be determined. Secondary aminated antidepressants (desipramine and nortriptyline) were more potent inhibitors than their tertiary aminated analogues (imipramine, chlorimipramine and amitriptyline). All drugs tested, except desipramine decreased the rate of firing of the serotonergic cells. In this case, the tertiary aminated antidepressants were much more potent than their secondary analogues. Mianserin was only active at very high doses. These results are in good agreement with the relative potencies of the tricyclic antidepressants for blocking the uptake of noradrenaline and serotonin into central and peripheral neurons.
在水合氯醛麻醉的大鼠中，用细胞外微电极记录蓝斑去甲肾上腺素能神经元和中缝背核5-羟色胺能神经元的自发放电率。对五种三环类抗抑郁药、反苯环丙胺和米安色林对这两类细胞自发放电活动的影响进行了定量比较。除米安色林外，所有受试药物均降低了去甲肾上腺素能神经元的放电频率。静脉灌注药物可确定抑制放电至基线率的50%（ID50）所需的剂量。仲胺类抗抑郁药（地昔帕明和去甲替林）比叔胺类类似物（丙咪嗪、氯米帕明和阿米替林）是更强效的抑制剂。除地昔帕明外，所有受试药物均降低了5-羟色胺能细胞的放电率。在这种情况下，叔胺类抗抑郁药比其仲胺类类似物强效得多。米安色林仅在非常高的剂量下才有活性。这些结果与三环类抗抑郁药阻断去甲肾上腺素和5-羟色胺摄取到中枢和外周神经元中的相对效力非常一致。
