Prostaglandin E2 binding sites in porcine oxyntic mucosa: effects of salicylates.
These studies were designed to examine the changes in the characteristics of prostaglandin E2 (PGE2) binding to porcine oxyntic mucosa in the response to oral ingestion of salicylates. Either acetylsalicylic acid (ASA) or salicylic acid (SA) was administered to conscious pigs (100 mg/kg in 30 mL of an equimolar concentration of NaHCO3) once a day for 1, 3, 10, or 20 days. In control experiments a similar volume of 0.3 M NaHCO3 was administered for similar durations. Mucosal ulceration and the characteristics of the binding of [3H]PGE2 to a 30 000 X g membrane preparation of oxyntic mucosa were examined. Generation of mucosal PGE2 was measured by radioimmunoassay. ASA treatment resulted in an increase in the number and severity of mucosal ulcers and a decrease in PGE2 levels within the first treatment day. By day 20 the degree of ulceration had decreased in spite of a persistent reduction of mucosal PGE2 generation. A variable degree of ulceration was observed in SA-treated animals. In control animals only a single class of binding sites for [3H]PGE2 was evident. After 3 days of ASA treatment a second class of binding sites with a high affinity dissociation constant appeared. There was a decrease in the high affinity binding of [3H]PGE2 after 20 days of ASA ingestion. Low affinity binding was not altered. ASA treatment resulted in a significant increase in specific binding capacities for both families of binding sites. SA treatment did not consistently alter PGE2 binding characteristics from control at any time period studied.(ABSTRACT TRUNCATED AT 250 WORDS)
Tepperman
B L
BL
Soper
B D
BD
D000818:Animals; D001241:Aspirin / Q000494:pharmacology*; D001665:Binding Sites / Q000187:drug effects; D015232:Dinoprostone; D005260:Female; D005753:Gastric Mucosa / Q000166:cytology* / Q000187:drug effects / Q000378:metabolism; D010295:Parietal Cells, Gastric / Q000378:metabolism*; D011458:Prostaglandins E / Q000096:biosynthesis / Q000378:metabolism*; D012459:Salicylates / Q000494:pharmacology*; D020156:Salicylic Acid; D013552:Swine; D014316:Tritium
D011458:Prostaglandins E; D012459:Salicylates; D014316:Tritium; D015232:Dinoprostone; D020156:Salicylic Acid; D001241:Aspirin