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首页> 外文期刊>Research communications in molecular pathology and pharmacology >Effects of various 5-HT3 receptor antagonists, granisetron, ondansetron, ramosetron and azasetron on serotonin (5-HT) release from the ferret isolated ileum.
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Effects of various 5-HT3 receptor antagonists, granisetron, ondansetron, ramosetron and azasetron on serotonin (5-HT) release from the ferret isolated ileum.

机译：各种5-HT3受体拮抗剂，格拉司琼，恩丹西酮，雷莫司琼和氮杂质子对从雪貂分离回肠释放的血清素（5-HT）的影响。

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摘要

The object of this study was to evaluate the involvement of 5-HT3 receptors in the regulation of 5-HT release from the small intestine using ferrets, an animal model of emesis. 2-Methyl-5-HT, a 5-HT3 receptor agonist, produced a concentration-dependent increase of 5-HT from the ferret ileum. This increase in 5-HT release was significantly inhibited by granisetron (10(-7) and 10(-6) M) or azasetron (10(-7) and 10(-6) M) in a concentration-dependent manner. Ondansetron (10(-7) M) and ramosetron (10(-6) M) also significantly inhibited the 2-methyl-5-HT-induced increase in 5-HT release. When the concentration of ondansetron was increased from 10(-7) M to 10(-6) M, inhibition of 5-HT release was reduced. Ramosetron, for which 5-HT3 receptor binding of the rat brain is remarkably stronger than for any other 5-HT3 receptor antagonists, inhibited the 5-HT release at only the highest concentration of 10(-6) M. Based on these observations that the mode of action on the 2-methyl-5-HT induced 5-HT release is different among 5-HT3 receptor antagonists, it is suggested that there is a possibility that the neuronal 5-HT3 receptors and the 5-HT3 receptors on the EC cells may represent two distinct subtypes.
机译：这项研究的目的是使用雪貂（一种呕吐的动物模型）评估5-HT3受体参与小肠5-HT释放的调节。 5-HT3受体激动剂2-甲基-5-HT从雪貂回肠产生了5-HT浓度依赖性的增加。 5-HT释放的这种增加以浓度依赖的方式被granisetron（10（-7）和10（-6）M）或azasetron（10（-7）和10（-6）M）显着抑制。恩丹西酮（10（-7）M）和雷莫司琼（10（-6）M）也显着抑制2-甲基-5-HT诱导的5-HT释放增加。当恩丹西酮的浓度从10（-7）M增加到10（-6）M时，对5-HT释放的抑制作用降低。 Ramosetron的大鼠脑中5-HT3受体的结合力明显强于任何其他5-HT3受体拮抗剂，在仅10（-6）M的最高浓度下就抑制了5-HT的释放。基于这些观察， 5-HT3受体拮抗剂之间对2-甲基-5-HT诱导的5-HT释放的作用方式不同，这提示神经元5-HT3受体和5-HT3受体可能存在EC细胞可能代表两种不同的亚型。

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