Antiulcer activity of pentacaine and some of its derivatives: effect on experimentally induced gastric and duodenal lesions and on gastric acid secretion in rats.

The antiulcer, gastroprotective, and antisecretory effects of selected carbanilates were tested in rats. The compounds K-1905 and K-2002 were found to have beneficial effects similar to those of pentacaine in phenylbutazone- and ethanol-induced gastric injury and in cysteamine-induced duodenal lesions; their antisecretory activity was also comparable to pentacaine in pylorus-ligated rats. Compounds P2 and P3 were generally less effective than pentacaine, and compound P1 was gastrotoxic. Thus pentyloxy-substitution on the benzene ring of the parent structure (K-1905 and K-2002) is more suitable for antiulcer and gastroprotective activity than methoxy-substitution on the meta-position (P3) or alkyloxy-substitution on the para-position (P2, P1). The results indicate that the two carbanilates K-1905 and K-2002 can be considered prospective antiulcer drugs.