Goicoechea C, Ormazábal M J, Alfaro M J, Martín M I
Dpto. Farmacología, Facultad de Medicina, Universidad Complutense de Madrid, Spain.
Neurosci Lett. 1999 Feb 26;262(1):25-8. doi: 10.1016/s0304-3940(99)00028-2.
The analgesic effect of three different opioid agonists, DAMGO ([D-Ala2,N-Me-Phe4,Gly5-ol]enkephalin), U-50,488H (trans-3,4-dichloro-N-methyl-N-[2-(1-pyrrolidynyl)cyclohexyl] benzene-aceramide methane sulphonate), and [D,Pen2-D,Pen5]-enkephalin, which act upon mu, delta and kappa opioid receptors, respectively, was compared in the presence and absence of salmon-calcitonin (s-CT). The analgesic test used was the writhing test in mice. The analgesic effect of the opioids was significantly enhanced by pretreatment of the animals with s-CT intraperitoneally (i.p.) administered. This effect was more evident for the delta and kappa-agonists. The present result suggests that the joint administration of s-CT and opioids may be a useful and interesting alternative in the treatment of painful diseases resistant to other treatments.
分别作用于μ、δ和κ阿片受体的三种不同阿片类激动剂,即DAMGO([D-丙氨酸2,N-甲基苯丙氨酸4,甘氨酸5-醇]脑啡肽)、U-50,488H(反式-3,4-二氯-N-甲基-N-[2-(1-吡咯烷基)环己基]苯-乙酰胺甲磺酸盐)和[D-青霉胺2,D-青霉胺5]-脑啡肽,在有和没有鲑鱼降钙素(s-CT)的情况下进行了镇痛效果比较。所采用的镇痛试验是小鼠扭体试验。通过腹腔内(i.p.)给予动物s-CT进行预处理,可显著增强阿片类药物的镇痛效果。这种作用对δ和κ激动剂更为明显。目前的结果表明,联合使用s-CT和阿片类药物可能是治疗对其他治疗有抗性的疼痛性疾病的一种有用且有趣的替代方法。