7-Oxo-prostaglandin E_1 Analogsのラットにおけるインドメサシン潰瘍抑制作用

概要

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The synthetic prostaglandin, 7-oxo-prostaglandin E_1 analogs were tested for prevention of ulcer formation induced by indomethacin in rat, and its structure-activity relationship was studied. 7-Oxo-15-methyl prostaglandin E_1 methyl ester (TEI-1226) was the most potent compound of the analogs when given orally. The prevention of indomethacin induced gastrointestinal lesion by TEI-1226 was about 2 times more potent than that by PG E_2,while the potency of diarrhea induction by TEI-1226 was almost equivalent to that of PG E_2. Prostaglandin-like activity of TEI-1226 on smooth muscles (rabbit aorta, guinea-pig trachea, rat stomach, and rat colon) was about 100 times less active than that of PG F_<2a> or PG E_2. In conclusion, synthetic 7-oxo-PG E_1 analogs appeared to be useful in the treatment for the gastric side effect caused by nonsteroidal anti-inflammatory drugs.
社団法人日本薬学会の論文
1981-03-25