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目的：观察胍丁胺对吗啡耐受和物质依赖豚鼠回肠纵肌（ＧＰＩＬＭ）的作用．方法：本实验在离体电场刺激实验中进行．结果：吗啡抑制ＥＦＳ引起的ＧＰＩＬＭ收缩［ＩＣ５０＝１４０（１０７－１８２）ｎｍｏｌ·Ｌ－１］．用吗啡２７０ｎｍｏｌ·Ｌ－１与ＧＰＩＬＭ温浴使吗啡ＩＣ５０增大３７倍（耐受），对纳络酮发生收缩反应（物质依赖）．分别用吗啡加纳络酮和吗啡加胍丁胺与ＧＰＩＬＭ温浴使吗啡失去此致耐受作用，使标本对纳络酮收缩反应幅度分别减少了９０％和７５％．胍丁胺的这些作用几乎可被咪唑克生完全阻断．结论：胍丁胺通过激活咪唑啉受体抑制离体ＧＰＩＬＭ对吗啡耐受和物质依赖的形成过程
Objective: To observe the effect of agmatine on morphine tolerance and substance dependent guinea pig ileum longitudinal muscle (GPILM). Methods: The experiment in vitro stimulation experiments. RESULTS: Morphine inhibited EFS-induced GPILM contractions [IC50 = 140 (107-182) nmol·L-1]. With morphine 270nmol·L-1 and GPILM warm bath, the IC50 of morphine increased by 37 times (tolerance), the contraction reaction of naloxone (substance-dependent). Morphine and morphine plus agmatine and GPILM were used respectively to inactivate morphine tolerance and reduce the amplitude of naloxone contraction by 90% and 75% respectively. These effects of agmatine are almost completely blocked by imidazole. CONCLUSIONS: Agmatine inhibits the morphine tolerance and substance-dependent formation of ex vivo GPILM by activating imidazolinium receptors