Some pharmacological actions of nisoxetine, a bicyclic inhibitor of noradrenaline uptake.
Some pharmacological actions of nisoxetine, a bicyclic inhibitor of noradrenaline uptake.
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尼索西汀（一种去甲肾上腺素摄取双环抑制剂）的一些药理作用。
DOI：
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发表时间：
1985
期刊：
影响因子：
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通讯作者：
Pennefather Jn
中科院分区：
文献类型：
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作者：
Leedham Ja;Foley Aj;Pennefather Jn
苯氧基苯丙胺（nisoxetine）的某些外周作用已与三环类抗抑郁药地昔帕明（desipramine）进行了比较。这两种药物在抑制大鼠输精管的交感神经末梢的3 H-去甲肾上腺素的积累方面是等效的;并且，在低剂量下，在增强该组织中α 1-和α 2-肾上腺素受体的去甲肾上腺素的作用方面是等效的。在输精管，α 1-肾上腺素能受体阻断作用的地昔帕明是明显的浓度为0.1 μ mol L-1及以上; nisoxetine是不太有效的。两种药物均未对α 2-肾上腺素受体表现出拮抗作用。尼索西汀在抑制豚鼠离体回肠对组胺、卡巴胆碱和缓激肽的反应方面也不如地昔帕明有效。因此，nisoxetine是更具体的两个神经元摄取抑制剂，并可能是一个有用的工具，以阻止神经元摄取的实验设计分类肾上腺素受体在其他组织。
Some peripheral actions of the phenoxyphenylpropylamine, nisoxetine, have been compared with those of the tricyclic antidepressant, desipramine. The two drugs were equipotent in inhibiting the accumulation of 3H-noradrenaline by the sympathetic nerve terminals of the rat vas deferens; and, in low doses, equipotent in potentiating the actions of noradrenaline at both alpha 1- and alpha 2-adrenoceptors in this tissue. In the vas deferens, the alpha 1-adrenoceptor blocking action of desipramine was evident at concentrations of 0.1 mumol l-1 and above; nisoxetine was less potent. Neither drug exhibited antagonist actions at alpha 2-adrenoceptors. Nisoxetine was also less potent than desipramine in inhibiting responses to histamine, carbachol and bradykinin on the guinea-pig isolated ileum. Thus nisoxetine is the more specific of the two neuronal uptake inhibitors and may be a useful tool to block neuronal uptake in experiments designed to classify adrenoceptors in other tissues.