首页> 美国卫生研究院文献>British Journal of Pharmacology and Chemotherapy >Uptake and release of 5-hydroxytryptamine by enteric 5-hydroxytryptaminergic neurones: effects of fluoxetine (Lilly 110140) and chlorimipramine.
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Uptake and release of 5-hydroxytryptamine by enteric 5-hydroxytryptaminergic neurones: effects of fluoxetine (Lilly 110140) and chlorimipramine.

机译:肠内5-羟色胺能神经元摄取和释放5-羟色胺:氟西汀(Lilly 110140)和氯丙咪嗪的作用。

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摘要

The effect of fluoxetine on uptake of 5-hydroxytryptamine (5-HT) by enteric 5-hydroxytryptaminergic neurones has been analyzed in order to compare further these neurones with 5-HT neurones of the CNS. In addition, the effects of fluoxetine and chlorimipramine on efflux of [3H]-5-HT from the myenteric plexus were also evaluated. Fluoxetine was found to be a competitive inhibitor of 5-HT uptake by the myenteric plexus and was a more potent inhibitor of 5-HT uptake than was chlorimipramine. However, chlorimipramine enhanced the efflux of [3H]-5-HT more than could be explained by inhibition of 5-HT uptake and, therefore, appears to have the additional action of releasing the amine. These observations, similar to those of others studying central neurones, support the view that enteric 5-HT neurones resemble those of the CNS and are a useful model for the evaluation of drugs.
机译:为了进一步比较这些神经元与中枢神经系统的5-HT神经元,已经分析了氟西汀对5-羟色胺肠溶性神经元摄取5-羟色胺(5-HT)的影响。此外,还评估了氟西汀和氯丙咪嗪对肌间神经丛[3H] -5-HT流出的影响。氟西汀被发现是一种肌间神经丛对5-HT摄取的竞争性抑制剂,并且是比氯丙咪嗪更有效的5-HT摄取抑制剂。然而,氯丙咪嗪增强[3H] -5-HT的流出比抑制5-HT吸收所解释的要多,因此似乎具有释放胺的附加作用。这些观察结果与其他研究中枢神经元的观察结果相似,支持以下观点:肠道5-HT神经元类似于中枢神经系统,并且是评估药物的有用模型。

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