1981 年 101 巻 3 号 p. 247-253
The synthetic prostaglandin, 7-oxo-prostaglandin E1 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 E1 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 E2, while the potency of diarrhea induction by TEI-1226 was almost equivalent to that of PG E2. 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 F2a or PG E2. In conclusion, synthetic 7-oxo-PG E1 analogs appeared to be useful in the treatment for the gastric side effect caused by nonsteroidal anti-inflammatory drugs.