Abstract
The influence of transposing the C-15 hydroxy group of prostaglandin E 1 methyl ester (PGE 1ME) on gastric antisecretory and antiulcer actions was investigated. The compound (±)15-deoxy- 16α,β-hydroxy PGE 1ME (SC-28904) was equipotent to the reference standard PGE 1ME in suppressing histamine-stimulated gastric secretion in the Heidenhain pouch (HP) dog. In contrast to PGE 1ME, SC-28904 was longer acting when administered intravenously and also showed significant oral activity in the histamine-stimulated gastric fistula dog. SC-28904 was also equipotent to PGE 1ME (range of active doses of 0.5 to 5.0 mg/kg, s.c.) in inhibiting forced-exertion gastric ulceration in rats. The compound (±)15-deoxy-17α,β-hydroxy PGE 1ME (SC-30693) was an inactive antisecretory agent in the dog at the 1.0 mg/kg i.v. bolus dose. This dose was 100 times greater than the active antisecretory dose of PGE 1ME. Likewise, SC-30693, when administered subcutaneously at a 5.0 mg/kg dose, was also totally inactive in preventing gastric ulcers induced by forced exertion in rats. The important implications of this work are that some of the receptor sites for the PGE 1 molecule could easily accommodate the side chain hydroxy group either in the C-15 or C-16 position. Moreover, the hydroxy group in the latter position significantly improved the biological activity of PGE 1ME.
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