PHARMACEUTICAL STUDIES ON ACONITUM ROOTS .18. MECHANISM OF ANALGESIC ACTION OF MESACONITINE .1. RELATIONSHIP BETWEEN ANALGESIC EFFECT AND CENTRAL MONOAMINES OR OPIATE RECEPTORS
PHARMACEUTICAL STUDIES ON ACONITUM ROOTS .18. MECHANISM OF ANALGESIC ACTION OF MESACONITINE .1. RELATIONSHIP BETWEEN ANALGESIC EFFECT AND CENTRAL MONOAMINES OR OPIATE RECEPTORS
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DOI：
10.1016/0014-2999(84)90027-x
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发表时间：
1984-01-01
影响因子：
5
通讯作者：
HIKINO, H
中科院分区：
文献类型：
--
作者：
MURAYAMA, M;ITO, T;HIKINO, H
本文用药理学和神经化学方法研究了中枢单胺和阿片受体对新乌头碱（MA）镇痛的作用，并以吗啡（莫尔）作对照。MA（i. c.）通过醋酸诱导的扭体法和甩尾法测定的活性是剂量依赖性的，表明其活性是通过CNS引起的。MA诱导的镇痛作用被α-SMA降低。甲基-p-酪氨酸（α- MT）、6-羟多巴胺、二乙基二硫代氨基甲酸盐、双硫仑和利血平，甲基苯丙胺和去甲肾上腺素（NE）可增加这些指标。MA的作用方式与莫尔相似，除了与左旋多巴、多巴胺、α-多巴胺联合给药后获得的结果不同MT或与5-羟色胺有关的化学品。MA促进了α- MT诱导的海马、延髓、脑桥和脊髓NE水平降低。左丙诺啡不影响MA的镇痛活性，表明其活性不通过阿片受体介导。显然，由MA介导的镇痛活性与涉及中枢儿茶酚胺能系统，特别是去甲肾上腺素能系统的反应密切相关。
The contribution of the central monoamines and the opiate receptor to mesaconitine (MA [from certain species of Aconitum plants])-induced analgesia was investigated by means of pharmacological and neurochemical methods in which morphine (Mor) was used for comparison. The analgesic action of MA (i.c.) determined by the acetic acid-induced writhing method and the tail flick method was dose-dependent, indicating that its activity is elicited through the CNS. MA-induced analgesia was decreased by .alpha.-methyl-p-tyrosine (.alpha.-MT), 6-hydroxydopamine, diethyldithiocarbamate, disulfiram and reserpine, and increased by methamphetamine and norepinephrine (NE). The mode of action of MA was similar to that of Mor except for the results obtained upon combined administration with L-dopa, dopamine, .alpha.-MT or chemicals related to 5-hydroxytryptamine. MA promoted the .alpha.-MT-induced decrease in NE levels in hippocampus, medulla oblongata plus pons and spinal cord. Levallorphan did not affect the analgesic activity of MA, showing that its activity is not mediated via the opiate receptors. Evidently, the analgesic activity mediated by MA is closely related to responses involving the central catecholaminergic system, in particular, the noradrenergic system.