Meyer G, Botta G, Tavani A, Algeri S, Cremaschi D
Dipartimento di Fisiologia e Biochimica Generali, Università di Milano, Italy.
J Pharm Pharmacol. 1989 Jul;41(7):494-5. doi: 10.1111/j.2042-7158.1989.tb06510.x.
The selective mu-opioid agonist [D-Ala2,MePhe4,Gly-ol5]enkephalin (DAGO) (10 microM) reduced the short circuit (Isc) and the L-valine induced increase of the transepithelial potential difference and Isc(delta Vms and delta Isc) measured in-vitro in rabbit ileum, with a mechanism antagonized by naloxone (1 microM). [D-Ala2,D-Leu5]enkephalin (DADLE) (10 microM) had no significant effect on the transepithelial potential difference (Vms), Isc, delta Vms and delta Isc. In the ileum deprived of the serosa and muscolaris, DAGO reduced the delta Vms and delta Isc, but not the Vms and Isc, suggesting localization of the receptors responsible for this latter effect in the myenteric plexus and/or the muscularis mucosae. These preliminary results suggest that in the rabbit ileum opioids influence electrolyte and amino acid transport and these effects may be at least partly mediated by mu-receptors.
选择性μ阿片受体激动剂[D-丙氨酸2,甲硫氨酸苯丙氨酸4,甘醇5]脑啡肽(DAGO)(10微摩尔)降低了短路电流(Isc)以及L-缬氨酸诱导的兔回肠体外测量的跨上皮电位差和Isc(ΔVms和ΔIsc)的增加,其机制可被纳洛酮(1微摩尔)拮抗。[D-丙氨酸2,D-亮氨酸5]脑啡肽(DADLE)(10微摩尔)对跨上皮电位差(Vms)、Isc、ΔVms和ΔIsc无显著影响。在去除浆膜和肌层的回肠中,DAGO降低了ΔVms和ΔIsc,但未降低Vms和Isc,提示负责后一种效应的受体定位于肌间神经丛和/或黏膜肌层。这些初步结果表明,在兔回肠中阿片类药物影响电解质和氨基酸转运,且这些效应可能至少部分由μ受体介导。