豚鼠回肠中阿片类药物作用评估的新模型。
New models for the evaluation of opioid effects in the guinea-pig ileum.
作者信息
Donnerer J, Lembeck F
出版信息
Br J Pharmacol. 1985 May;85(1):61-4. doi: 10.1111/j.1476-5381.1985.tb08831.x.
The pharmacology of morphine and opioid peptides was studied in the guinea-pig ileum by examining their inhibitory effects on propulsive peristaltic activity and on the cooling-induced longitudinal contraction. In these experiments, dose-response curves were recorded. The rank order of potency in inhibiting peristalsis was found to be: dermorphin greater than FK 33-824 greater than dynorphin-(1-17) greater than dynorphin-(1-13) greater than delta-receptor-peptide greater than morphine greater than [Leu] enkephalin, whereas the rank order in inhibiting cooling-induced contractions was found to be: dynorphin-(1-13) congruent to FK 33-824 congruent to dermorphin greater than delta-receptor peptide greater than morphine. Naloxone antagonized the maximally effective dose of each of the opioid agents. In view of the differences between the abilities of these opioids to inhibit propulsive peristaltic activity, these models seem to be valuable for the examination of inhibitory opioid effects in the gut.
通过检测吗啡和阿片肽对豚鼠回肠推进性蠕动活动及冷诱导纵向收缩的抑制作用，对它们的药理学特性进行了研究。在这些实验中，记录了剂量-反应曲线。结果发现，抑制蠕动的效力顺序为：皮啡肽＞FK 33-824＞强啡肽-(1-17)＞强啡肽-(1-13)＞δ-受体肽＞吗啡＞亮氨酸脑啡肽，而抑制冷诱导收缩的效力顺序为：强啡肽-(1-13)≈FK 33-824≈皮啡肽＞δ-受体肽＞吗啡。纳洛酮可拮抗每种阿片类药物的最大有效剂量。鉴于这些阿片类药物抑制推进性蠕动活动的能力存在差异，这些模型似乎对于研究肠道中阿片类药物的抑制作用具有重要价值。
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