Rozé C, Dubrasquet M, Chariot J, Vaille C
Eur J Pharmacol. 1982 Mar 12;78(3):271-8. doi: 10.1016/0014-2999(82)90028-0.
Pancreatic and gastric secretions after stimulation with acetylcholine, electrical vagal stimulation or 2-deoxyglucose injection were studied in anesthetized rats. The effects of methadone on these secretions were investigated. Maximal stimulation of pancreatic secretion by acetylcholine was not affected by methadone. Gastric acid stimulation by acetylcholine was only slightly decreased by methadone (30% or less). Electrical vagal stimulation of pancreatic and gastric secretions was progressively and dose-dependently decreased to a maximum of 50% by methadone. Maximal stimulation of pancreatic and gastric secretions by 2-deoxyglucose was completely suppressed by methadone with an ID50 of about 1 mg/kg and an ID100 of about 2.5 mg/kg for both secretions. It is concluded that methadone inhibits vagal stimulation of digestive secretions by acting both centrally and peripherally (probably by inhibiting the release of acetylcholine from vagal fibers). The central mechanism appears to be more important, since it occurs with lower doses and can produce complete suppression of secretion.
在麻醉大鼠中研究了用乙酰胆碱、电迷走神经刺激或注射2-脱氧葡萄糖刺激后的胰腺和胃分泌物。研究了美沙酮对这些分泌物的影响。乙酰胆碱对胰腺分泌的最大刺激不受美沙酮影响。乙酰胆碱对胃酸的刺激仅略微被美沙酮降低（30%或更低）。美沙酮使电迷走神经刺激胰腺和胃分泌物逐渐且剂量依赖性地降低，最大降低至50%。2-脱氧葡萄糖对胰腺和胃分泌的最大刺激被美沙酮完全抑制，两种分泌物的半数抑制剂量（ID50）约为1mg/kg，完全抑制剂量（ID100）约为2.5mg/kg。结论是美沙酮通过中枢和外周作用（可能是通过抑制迷走神经纤维释放乙酰胆碱）抑制迷走神经对消化分泌物的刺激。中枢机制似乎更重要，因为它在较低剂量时就会出现，并且可以完全抑制分泌。
