[The site (central or peripheral) of the anti-ulcer action of dalargin, a synthetic analog of endogenous opioids in an experimental model of cysteamine-induced duodenal ulcer in rats].
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.
D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage; D001921:Brain / Q000378:metabolism; D003543:Cysteamine / Q000633:toxicity; D004195:Disease Models, Animal; D004381:Duodenal Ulcer / Q000139:chemically induced / Q000517:prevention & control*; D004743:Enkephalin, Leucine / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D016308:Enkephalin, Leucine-2-Alanine / Q000031:analogs & derivatives; D007276:Injections, Intraventricular; D007279:Injections, Subcutaneous; D008297:Male; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects* / Q000378:metabolism
D000897:Anti-Ulcer Agents; D011957:Receptors, Opioid; D004743:Enkephalin, Leucine; D003543:Cysteamine; D016308:Enkephalin, Leucine-2-Alanine; C040996:enkephalin-Leu, Ala(2)-Arg(6)-
Mesto prilozheniia (tsentral'noe ili perifericheskoe) protivoiazvennogo deĭstviia sinteticheskogo analoga éndogennykh opioidov dalargina v éksperimental'noĭ modeli tsisteaminovykh duodenal'nykh iazv u krys.