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首页> 外文期刊>Canadian Journal of Physiology and Pharmacology >Doxazosin selectively potentiates contraction to serotonin via 5-HT2A receptors in longitudinal muscle strips of the rabbit gastric body
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Doxazosin selectively potentiates contraction to serotonin via 5-HT2A receptors in longitudinal muscle strips of the rabbit gastric body

机译：多沙唑嗪通过兔胃体纵肌条中的5-HT2A受体选择性增强5-羟色胺的收缩

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摘要

The aims of this study were to examine the effects of doxazosin on contractile responses to 5-hydroxytryptamine (5-HT), carbachol, and histamine, and to compare them with those of prazosin, alfuzosin, and terazosin, and then characterize a pharmacological profile of the 5-HT-induced contractile response using preparations of isolated longitudinal muscle strips from the rabbit gastric body. The results from these preparations showed that the contraction response to 5-HT, but not to carbachol or histamine, was found to be dose-dependently potentiated by doxazosin and its enantiomers. The specific potentiation effect on 5-HT was not observed in the preparations that were treated with prazosin, terazosin, or alfuzosin. The contractile response to 5-HT and its potentiation by doxazosin were not affected by treatment with phenoxybenzamine. However, 5-HTinduced contraction was competitively antagonized by nefazodone (with pA2 value of 8.64 ± 0.17), and was almost completely inhibited by treatment with indomethacin. In conclusion, doxazosin, but not prazosin, alfuzosin, or terazosin, selectively potentiates 5-HT-induced contraction in the rabbit gastric body strips via an α1-adrenoceptor-independent mechanism, without chiral recognition of its enantiomers. Additionally, the contraction to 5-HT was found to be mediated via 5-HT2A receptors, and was similar to PGs synthesis in the preparations.
机译：这项研究的目的是检查多沙唑嗪对5-羟色胺（5-HT），卡巴胆碱和组胺的收缩反应的作用，并将其与哌唑嗪，阿夫唑嗪和特拉唑嗪的收缩反应进行比较，然后描述其药理特性兔胃体中分离出的纵向肌条制备5-HT引起的收缩反应。这些制剂的结果表明，对多沙唑嗪及其对映体的剂量依赖性地增强了对5-HT而不是对卡巴胆碱或组胺的收缩反应。在用哌唑嗪，特拉唑嗪或阿夫唑嗪处理的制剂中未观察到对5-HT的特异性增强作用。苯氧基苯甲胺处理对5-HT的收缩反应及其多沙唑嗪的增强作用没有影响。然而，奈法唑酮竞争性拮抗5-HT引起的收缩（pA2值为8.64±0.17），吲哚美辛治疗几乎完全抑制了5-HT收缩。总之，多沙唑嗪而不是哌唑嗪，阿夫唑嗪或特拉唑嗪通过α1-肾上腺素受体独立机制选择性增强了5-HT诱导的兔胃体条带的收缩，而没有手性识别其对映体。另外，发现5-HT的收缩是通过5-HT 2A受体介导的，与制剂中PGs的合成相似。

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