Polonskiĭ V M, Iarygin K N, Krivosheev O G, Moskovkin G N, Vinogradov V A
Biull Eksp Biol Med. 1987 Apr;103(4):433-4.
Dalargin injected subcutaneously at a dose of 10 micrograms/kg decreased 4-5 fold ulcer manifestations in rats with cysteamine-induced duodenal ulcers. Intracerebroventricular dose of 2 micrograms diminished the manifestations to a lesser extent Dalargin only at a dose exceeding 500 micrograms intraperitoneally decreased significantly the in vivo binding of 3H-D-Ala2, D-Leu5-enkephalin with brain opiate receptors. We believe that Dalargin injected peripherally in small doses does not penetrate the blood-brain barrier and that its antiulcer activity is due to the interaction with peripheral opioid receptors. It seems possible that the disturbances in the central/peripheral ratio of the opioid activity plays an important role in the pathogenesis of duodenal peptic ulcer.
以10微克/千克的剂量皮下注射达乐argin可使半胱胺诱导的十二指肠溃疡大鼠的溃疡表现减少4至5倍。脑室内注射2微克的达乐argin在较小程度上减轻了溃疡表现。只有当腹腔注射剂量超过500微克时,达乐argin才会显著降低3H-D-丙氨酸2、D-亮氨酸5-脑啡肽与脑阿片受体的体内结合。我们认为,小剂量外周注射达乐argin不会穿透血脑屏障,其抗溃疡活性是由于与外周阿片受体相互作用所致。阿片活性的中枢/外周比例失调似乎在十二指肠消化性溃疡的发病机制中起重要作用。