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选择性5-羟色胺(5-HT)3受体激动剂对雪貂肠道蠕动的影响。

The effect of the selective 5-HT(3) receptor agonist on ferret gut motility.

作者信息

Nagakura Yukinori, Kiso Tetsuo, Miyata Keiji, Ito Hiroyuki, Iwaoka Kiyoshi, Yamaguchi Tokio

机构信息

Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd., 21 Miyukigaoka, Tsukuba, Ibaraki 305-8585, Japan.

出版信息

Life Sci. 2002 Aug 2;71(11):1313-9. doi: 10.1016/s0024-3205(02)01841-6.

Abstract

The effect of the selective 5-hydroxytryptamine (5-HT)(3) receptor agonist YM-31636 (2-(1H-imidazol-4-ylmethyl)-8H-indeno[1,2-d]thiazole monofumarate) on gut motility of fed ferrets was investigated. YM-31636 (0.1 mg/kg p.o.) induced a giant migrating contraction (GMC)-like, high-amplitude, ungrouped colonic contraction although it did not change the basal colonic motility pattern. This GMC-like contraction was always accompanied by defecation. Both GMC-like contraction and defecation were inhibited with the selective 5-HT(3) receptor antagonist ramosetron. YM-31636 affected gastric, duodenal and ileal motility pattern only slightly. These results suggest that 5-HT(3) receptor agonists such as YM-31636 are useful in treating constipation since they facilitate GMC-like contractions and defecation without undesired changes in gut motility pattern.

摘要

研究了选择性5-羟色胺(5-HT)(3)受体激动剂YM-31636(2-(1H-咪唑-4-基甲基)-8H-茚并[1,2-d]噻唑单富马酸盐)对喂食雪貂肠道运动的影响。口服0.1mg/kg的YM-31636可诱发类似巨移行收缩(GMC)的高振幅、非成组的结肠收缩,尽管它并未改变基础结肠运动模式。这种类似GMC的收缩总是伴有排便。选择性5-HT(3)受体拮抗剂雷莫司琼可抑制类似GMC的收缩和排便。YM-31636对胃、十二指肠和回肠运动模式的影响很小。这些结果表明,像YM-31636这样的5-HT(3)受体激动剂可用于治疗便秘,因为它们促进类似GMC的收缩和排便,而不会引起肠道运动模式的不良变化。

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