Burks T F, Hirning L D, Galligan J J, Davis T P
Life Sci. 1982;31(20-21):2237-40. doi: 10.1016/0024-3205(82)90127-8.
Six opioid peptides, like morphine, were found to produce dose-dependent contractions of dog isolated intestine when administered as intraarterial boluses. The increases in incidence and amplitude of intestinal contractions were antagonized by naloxone. The rank order of potency of the opioid agonists tested was D-Ala2-met-enkephalinamide greater than D-Ala2-leu-enkephalinamide greater than met-enkephalin greater than beta-endorphin 1-31 greater than morphine greater than morphiceptin greater than dynorphin 1-13. The contractions induced by two opioid agonists displayed differential sensitivity to blockade by tetrodotoxin (TTX). Met-enkephalin was barely affected by concentrations of TTX that markedly reduced responses to morphiceptin. Some portion of the motility effect of metenkephalin may be exerted directly on intestinal smooth muscle.
当以动脉内推注的方式给药时,发现六种阿片样肽(如吗啡)可使犬离体肠管产生剂量依赖性收缩。肠管收缩发生率和幅度的增加可被纳洛酮拮抗。所测试的阿片样激动剂的效价顺序为:D-丙氨酸²-甲硫氨酸脑啡肽酰胺>D-丙氨酸²-亮氨酸脑啡肽酰胺>甲硫氨酸脑啡肽>β-内啡肽1-31>吗啡>吗啡肽>强啡肽1-13。两种阿片样激动剂诱导的收缩对河豚毒素(TTX)阻断表现出不同的敏感性。甲硫氨酸脑啡肽几乎不受能显著降低对吗啡肽反应的TTX浓度的影响。甲硫氨酸脑啡肽的部分运动效应可能直接作用于肠道平滑肌。