Effect of trapencaine and some of its derivatives on gastric wall mucus in stressed rats.
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.
Nosálová
V
V
Institute of Experimental Pharmacology, Slovak Academy of Sciences, Bratislava.
Juránek
I
I
Babulová
A
A
D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D002219:Carbamates / Q000494:pharmacology*; D003080:Cold Temperature; D005260:Female; D005753:Gastric Mucosa / Q000187:drug effects / Q000378:metabolism*; D006471:Gastrointestinal Hemorrhage / Q000139:chemically induced; D009093:Mucus / Q000737:chemistry / Q000187:drug effects / Q000378:metabolism*; D051381:Rats; D017208:Rats, Wistar; D012149:Restraint, Physical; D013276:Stomach Ulcer / Q000517:prevention & control; D013315:Stress, Psychological / Q000378:metabolism*; D013329:Structure-Activity Relationship
D000779:Anesthetics, Local; D002219:Carbamates; C010618:pentacaine