Izzo A A, Mascolo N, Tonini M, Capasso F
Department of Experimental Pharmacology, University of Naples 'Federico II', via D. Montesano 49, 80131 Naples, Italy.
Br J Pharmacol. 2000 Mar;129(5):984-90. doi: 10.1038/sj.bjp.0703116.
The effect of cannabinoid drugs on peristalsis in the guinea-pig ileum was studied. Peristalsis was induced by delivering fluid into the oral end of an isolated intestinal segment. Longitudinal muscle reflex contraction, threshold pressure and threshold volume to trigger peristalsis, compliance of the intestinal wall during the preparatory phase (a reflection of the resistance of the wall to distension) and maximal ejection pressure during the emptying phase of peristalsis were measured. The cannabinoid agonists WIN 55,212-2 (0.3 - 300 nM) and CP55,940 (0.3 - 300 nM) significantly decreased longitudinal muscle reflex contraction, compliance and maximal ejection pressure, while increased threshold pressure and volume to elicit peristalsis. These effects were not modified by the opioid antagonist naloxone (1 microM) and by the alpha-adrenoceptor antagonist phentolamine (1 microM). The inhibitory effect of both WIN 55,212-2 and CP55,940 on intestinal peristalsis was antagonized by the cannabinoid CB(1) receptor antagonist SR141716A (0.1 microM), but not by the cannabinoid CB(2) receptor antagonist SR144528 (0.1 microM). In absence of other drugs, the CB(1) receptor antagonists SR141716A (0.01 - 1 microM) and AM281 (0.01 - 1 microM) slightly (approximatively 20%) but significantly increased maximal ejection pressure during the empty phase of peristalsis without modifying longitudinal muscle reflex contraction, threshold pressure, threshold volume to trigger peristalsis and compliance. It is concluded that activation of CB(1) receptors reduces peristalsis efficiency in the isolated guinea-pig, and that the emptying phase of peristalsis could be tonically inhibited by the endogenous cannabinoid system.
研究了大麻素类药物对豚鼠回肠蠕动的影响。通过向离体肠段的口腔端注入液体来诱发蠕动。测量了纵向肌反射收缩、触发蠕动的阈压力和阈体积、准备阶段肠壁的顺应性(反映肠壁对扩张的阻力)以及蠕动排空阶段的最大喷射压力。大麻素激动剂WIN 55,212-2(0.3 - 300 nM)和CP55,940(0.3 - 300 nM)显著降低纵向肌反射收缩、顺应性和最大喷射压力,同时增加触发蠕动的阈压力和阈体积。这些作用不受阿片类拮抗剂纳洛酮(1 microM)和α-肾上腺素能受体拮抗剂酚妥拉明(1 microM)的影响。WIN 55,212-2和CP55,940对肠道蠕动的抑制作用被大麻素CB(1)受体拮抗剂SR141716A(0.1 microM)拮抗,但未被大麻素CB(2)受体拮抗剂SR144528(0.1 microM)拮抗。在无其他药物存在时,CB(1)受体拮抗剂SR141716A(0.01 - 1 microM)和AM281(0.01 - 1 microM)在蠕动排空阶段轻微(约20%)但显著增加最大喷射压力,而不改变纵向肌反射收缩、阈压力、触发蠕动的阈体积和顺应性。得出结论:CB(1)受体的激活降低了离体豚鼠的蠕动效率,并且蠕动的排空阶段可能受到内源性大麻素系统的紧张性抑制。