Departments of Animal Health Human Anatomy, Pharmacology and Medico-Forensic Sciences, University of Parma, Italy.
Equine Vet J. 2012 May;44(3):368-70. doi: 10.1111/j.2042-3306.2011.00426.x. Epub 2011 Aug 23.
The effects of preferential µ (morphine), selective µ (fentanyl), selective κ (compound U69593) opioid receptor agonists, and nonselective (naloxone) and selective µ (naloxonazine) antagonists on equine small intestinal motility were evaluated in vitro. Samples of circular muscle from equine jejunum were placed in isolated organ baths and drug-induced modifications of both spontaneous and electrically evoked contractile activity were measured. None of the opioid agonists induced a significant change in spontaneous contractions. Fentanyl and U69593 reduced electrically induced contractions, whereas morphine reduced them only slightly. Naloxone competitively antagonised U69593, but both naloxone and naloxonazine were unable to counteract the inhibition of contractions induced by fentanyl. The inhibition of contractions shown by fentanyl is therefore probably not mediated by opioid receptors, but due to an anticholinergic activity of this drug. In summary, these data showed an inhibitory effect exerted by κ receptors on equine small intestinal motility, whereas the role of µ receptors seemed marginal and would need further characterisation.
在体外评估了优先µ(吗啡)、选择性µ(芬太尼)、选择性κ(化合物 U69593)阿片受体激动剂,以及非选择性(纳洛酮)和选择性µ(纳洛酮嗪)拮抗剂对马小肠运动的影响。从马空肠中取出环形肌样本,置于分离式器官浴中,并测量自发和电诱发收缩活动的药物诱导变化。阿片受体激动剂均未引起自发收缩的显著变化。芬太尼和 U69593 减少了电诱发的收缩,而吗啡仅轻微减少了收缩。纳洛酮竞争性拮抗 U69593,但纳洛酮和纳洛酮嗪均无法对抗芬太尼引起的收缩抑制。因此,芬太尼引起的收缩抑制可能不是由阿片受体介导的,而是由于该药物的抗胆碱能活性。总之,这些数据显示κ受体对马小肠运动产生抑制作用,而µ受体的作用似乎微不足道,需要进一步表征。