The effect of selected carbanilates on the rat gastric mucus was tested after oral administration. The compounds K 1905 and K 2002 were found to increase gastric mucus content in nonstressed rats while compound P 2 was ineffective. The activity of K 1905 was comparable with that of the parent drug trapencaine. Cold-restraint stress decreased the gastric mucus content and induced haemorrhagic erosions in the glandular stomach. With the exception of compound P 2 pretreatment with carbanilates dose-dependently diminished the extent of stress-induced gastric damage and prevented the depletion of mucus after stress. The results indicate that pentyloxy-substitution in the meta and in the para position on the benzene ring of the parent structure (K 1905 and K 2002, respectively) seems to be more suitable for mucus enhancing activity than alkyloxy-substitution on the para position (P 2). The observed increased mucus secretion might be partly responsible for the gastroprotective action of the drugs tested.

01 Mar 1993·Die Pharmazie

Comparison of local anesthetic activity of pentacaine (trapencaine) and some of its derivatives by three different techniques.

Article

Author: Stolc, S ; Mai, P M

The local anesthetic potency of the carbanilic drug pentacaine (1; trapencaine) was compared to that of a series of its derivatives as well as procaine and cocaine. It is known that 1 exhibits potent local anesthetic, gastroprotective and antiulcer activities. The local anesthetic potency of the drugs under study was tested by three different techniques, i.e. analysis of compound action potential amplitude in rat sciatic nerve in vitro, duration of full anesthesia in rabbit cornea in vivo as well as in guinea-pig skin in vivo. The potency was expressed as drug concentration evoking either 50% reduction in action potential amplitude in the isolated nerve or anesthesia lasting for 20 min in the other two techniques. The most powerful anesthetics were found to be 1, K1905, and K2002 with their potency exceeding that of procaine and cocaine by 1-2 orders. The derivatives P1, P2, and P3 were much less effective, their potency being comparable to the two reference drugs. Although there were remarkable differences in the ranges of effective concentrations of particular drugs in the techniques used, a comparatively good agreement was found in the orders of the drug potencies. Plotting local anesthetic potency and drug lipophilicity revealed a good positive correlation between these two parameters in the group of the drugs tested.

Methods and findings in experimental and clinical pharmacology

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

Article

Author: Bauer, V ; Nosálová, V ; Mai, M P ; Babulová, A

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.

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Indication	Highest Phase	Country/Location	Organization	Date
Peptic Ulcer	Preclinical	Slovakia	-	-

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