PT  - JOURNAL ARTICLE
AU  - W E Perkins
AU  - E G Burton
AU  - B S Tsai
AU  - P W Collins
AU  - J J Casler
AU  - A F Gasiecki
AU  - R F Bauer
AU  - P H Jones
AU  - T S Gaginella
TI  - SC-46275: a potent, long-acting gastric antisecretory prostaglandin with low oral bioavailability in the dog.
DP  - 1991 Dec 01
TA  - Journal of Pharmacology and Experimental Therapeutics
PG  - 1004--1007
VI  - 259
IP  - 3
4099  - http://jpet.aspetjournals.org/content/259/3/1004.short
4100  - http://jpet.aspetjournals.org/content/259/3/1004.full
SO  - J Pharmacol Exp Ther1991 Dec 01; 259
AB  - The synthetic prostaglandin, SC-46275, an omega chain cyclopentenyl analog of enisoprost, was studied to determine its gastric antisecretory potency and duration of action in meal-stimulated innervated (Pavlov) pouch dogs and its p.o. bioavailability in unoperated fasted dogs. SC-46275 exhibited potent antisecretory activity when administered directly into the gastric pouch, the ED50 being 0.01 micrograms/kg. It had a long duration of antisecretory action; significant (P less than or equal to .05) inhibition of total acid output was observed 16 hr after intrapouch administration of 0.03 micrograms/kg. At this dose p.o., neither SC-46275 nor its free acid metabolite was detected in plasma. These data indicate that SC-46275 has novel properties: it is a potent, long-acting gastric antisecretory agent which is not readily available systemically after p.o. administration. Thus, potential systemic side effects are expected to be absent or minimized at doses of SC-46275 which inhibit gastric acid secretion, and therefore it might be useful in peptic ulcer disease.