Martín M I, Alfaro M J, Goicoechea C, Colado M I
Departamento de Farmacología, Facultad de Medicina, Universidad Complutense de Madrid, Spain.
Naunyn Schmiedebergs Arch Pharmacol. 1993 Mar;347(3):324-8. doi: 10.1007/BF00167452.
A possible interaction of salmon-calcitonin with opioid systems was studied in isolated tissues. Neurogenic contractions were elicited by electrical stimulation in guinea-pig ileum myenteric plexus-longitudinal muscle strips, rabbit vas deferens and mouse vas deferens. Bremazocine inhibited neurogenic contractions in all three tissues (presumably through kappa-receptors) [D-Pen2, D-Pen5]enkephalin and [Met5]enkephalin inhibited contractions in mouse vas deferens (presumably through delta-receptors), and [D-Ala2, N-Me-Phe4, Gly5-ol]enkephalin (DAMGO) inhibited contractions in guinea-pig ileum and mouse vas deferens (presumably through mu-receptors). All inhibitory effects were concentration-dependent. Salmon-calcitonin 0.1 IU/ml increased the effect of bremazocine in guinea-pig ileum and rabbit vas deferens and also increased the effects of [D-Pen2, D-Pen5]enkephalin and [Met5]enkephalin in mouse vas deferens. In contrast, salmon-calcitonin up to 0.4 IU/ml did not change the effect of bremazocine in mouse vas deferens and the effect of DAMGO in guinea-pig ileum and mouse vas deferens. It is concluded that salmon-calcitonin enhances agonist effects at opioid kappa- and delta- but not at opioid mu-receptors. The level of this interaction remains to be elucidated. The interaction may be the basis of the analgesic effect of salmon-calcitonin in vivo.
在离体组织中研究了鲑鱼降钙素与阿片样物质系统之间可能的相互作用。通过电刺激豚鼠回肠肌间神经丛 - 纵肌条、兔输精管和小鼠输精管引发神经源性收缩。布瑞马唑辛抑制所有这三种组织中的神经源性收缩(可能通过κ受体);[D - Pen2,D - Pen5]脑啡肽和[Met5]脑啡肽抑制小鼠输精管中的收缩(可能通过δ受体),并且[D - Ala2,N - Me - Phe4,Gly5 - ol]脑啡肽(DAMGO)抑制豚鼠回肠和小鼠输精管中的收缩(可能通过μ受体)。所有抑制作用均呈浓度依赖性。0.1 IU/ml的鲑鱼降钙素增强了布瑞马唑辛在豚鼠回肠和兔输精管中的作用,也增强了[D - Pen2,D - Pen5]脑啡肽和[Met5]脑啡肽在小鼠输精管中的作用。相比之下,高达0.4 IU/ml的鲑鱼降钙素并未改变布瑞马唑辛在小鼠输精管中的作用以及DAMGO在豚鼠回肠和小鼠输精管中的作用。得出的结论是,鲑鱼降钙素增强阿片样物质κ和δ受体而非μ受体处的激动剂作用。这种相互作用的程度仍有待阐明。这种相互作用可能是鲑鱼降钙素在体内镇痛作用的基础。