肠道5-羟色胺能神经元对5-羟色胺的摄取与释放：氟西汀（礼来110140）和氯米帕明的作用
Uptake and release of 5-hydroxytryptamine by enteric 5-hydroxytryptaminergic neurones: effects of fluoxetine (Lilly 110140) and chlorimipramine.
作者信息
Gershon M D, Jonakait G M
出版信息
Br J Pharmacol. 1979 May;66(1):7-9. doi: 10.1111/j.1476-5381.1979.tb16089.x.
Abstract
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.
摘要
为了进一步比较肠内5-羟色胺能神经元与中枢神经系统5-羟色胺（5-HT）神经元，分析了氟西汀对肠内5-羟色胺能神经元摄取5-羟色胺（5-HT）的影响。此外，还评估了氟西汀和氯米帕明对[3H]-5-HT从肌间神经丛流出的影响。发现氟西汀是肌间神经丛摄取5-HT的竞争性抑制剂，并且是比氯米帕明更有效的5-HT摄取抑制剂。然而，氯米帕明增强[3H]-5-HT流出的程度超过了抑制5-HT摄取所能解释的程度，因此，似乎具有释放胺的额外作用。这些观察结果与其他研究中枢神经元的结果相似，支持了肠内5-HT神经元类似于中枢神经系统神经元且是评估药物的有用模型的观点。
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