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秋水仙碱诱导的平滑肌致敏:它是抗微管蛋白药物的体外特性吗?

Smooth muscle sensitization induced by colchicine: is it an in vitro property of antitubulin agents?

作者信息

Famaey J P, Fontaine J, Reuse J

出版信息

Agents Actions. 1977 Jul;7(2):305-9. doi: 10.1007/BF01969989.

Abstract

Colchicine 0.1 microgram/ml induces a reversible increase of guinea-pig isolated ileum contractions (50 to 60% of maximal contractions) to acetylcholine, nicotine and PGE2. At 1 microgram/ml, it induces an irreversible increase of similar contractions to acetylcholine and 5-hydroxytryptamine. Low concentrations of indomethacin are able to reduce or even to abolish this increase. This smooth muscle sensitization could be related to the ability of colchicine to stimulate prostaglandin biosynthesis. Vinblastine has been described to induce a similar in vitro sensitization of guinea-pig isolated ileum. This effect might be also a non-specific property of antitubulin agents. The relationships between such an in vitro sensitization and the clinical effects of colchicine, including diarrhea, remain unclear.

摘要

秋水仙碱0.1微克/毫升可使豚鼠离体回肠对乙酰胆碱、尼古丁和前列腺素E2的收缩反应出现可逆性增强(达到最大收缩反应的50%至60%)。在1微克/毫升时,它可使豚鼠离体回肠对乙酰胆碱和5-羟色胺的类似收缩反应出现不可逆增强。低浓度的吲哚美辛能够减轻甚至消除这种增强反应。这种平滑肌致敏作用可能与秋水仙碱刺激前列腺素生物合成的能力有关。据描述,长春碱可在体外诱导豚鼠离体回肠出现类似的致敏作用。这种效应可能也是抗微管蛋白药物的一种非特异性特性。这种体外致敏作用与秋水仙碱的临床效应(包括腹泻)之间的关系仍不清楚。

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