Bubenik G A
J Pineal Res. 1986;3(1):41-54. doi: 10.1111/j.1600-079x.1986.tb00725.x.
A dose-dependent increase in tone and reduction in amplitude of contractions was observed after serotonin (5-HT) was administered to isolated segments of rat ileum, incubated in Locke's solution at 38 degrees C. Melatonin (M) reduced the tone but not the amplitude or frequency of contractions. Addition of M (administered in doses 20 to 100 X higher than 5-HT) relieved the spasm induced by 5-HT. Furthermore, pretreatment with M significantly reduced the 5-HT effect. N-acetylserotonin (NAS) exhibited delayed but similar effect to M. Neither M nor NAS could prevent or relieve acetylcholine-induced contractions or influence relief of intestinal contractions by adrenaline. This indicates that 5-HT and M act via a different mechanism than that of adrenaline and acetycholine system. Serotonin muscle receptor blocker methysergide reduced 5-HT effect but was not able to abolish it completely. As methysergide could not reduce the muscle tone and did not relieve spasm caused by 5-HT, it is speculated that M is not acting as antagonist of 5-HT-stimulatory receptors but rather as agonist of 5-HT-inhibiting neuronal receptors.
在38摄氏度的洛克溶液中孵育的大鼠离体回肠段给予血清素(5-羟色胺,5-HT)后,观察到收缩张力呈剂量依赖性增加,收缩幅度降低。褪黑素(M)降低了张力,但未降低收缩幅度或频率。添加M(给予的剂量比5-HT高20至100倍)可缓解5-HT诱导的痉挛。此外,用M预处理可显著降低5-HT的作用。N-乙酰血清素(NAS)表现出延迟但与M相似的作用。M和NAS均不能预防或缓解乙酰胆碱诱导的收缩,也不影响肾上腺素对肠道收缩的缓解作用。这表明5-HT和M的作用机制与肾上腺素和乙酰胆碱系统不同。血清素肌肉受体阻滞剂麦角新碱降低了5-HT的作用,但不能完全消除它。由于麦角新碱不能降低肌张力,也不能缓解5-HT引起的痉挛,推测M不是作为5-HT刺激受体的拮抗剂起作用,而是作为5-HT抑制性神经元受体的激动剂起作用。