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.
Nosálová
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V
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava, Slovak Republic.
Mai
M P
MP
Babulová
A
A
Bauer
V
V
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000009:adverse effects; D000897:Anti-Ulcer Agents / Q000494:pharmacology*; D002219:Carbamates / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D003543:Cysteamine / Q000009:adverse effects; D004195:Disease Models, Animal; D004305:Dose-Response Relationship, Drug; D004381:Duodenal Ulcer / Q000139:chemically induced / Q000188:drug therapy*; D000431:Ethanol / Q000009:adverse effects; D005260:Female; D005744:Gastric Acid / Q000378:metabolism*; D010653:Phenylbutazone / Q000009:adverse effects; D048448:Phenylcarbamates; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000139:chemically induced / Q000188:drug therapy*; D013329:Structure-Activity Relationship
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000897:Anti-Ulcer Agents; D002219:Carbamates; D048448:Phenylcarbamates; C098556:2-diethylaminocyclopentyl 3-n-pentyloxyphenylcarbamate; D000431:Ethanol; D003543:Cysteamine; C010618:pentacaine; C098618:2-(1-pyrrolidinyl)cyclohexyl 4-pentyloxyphenylcarbamate; D010653:Phenylbutazone