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Titolo:
THE GASTRIN CHOLECYSTOKININ-B RECEPTOR ANTAGONIST L-365,260 REDUCES BASAL ACID-SECRETION AND PREVENTS GASTROINTESTINAL DAMAGE-INDUCED BY ASPIRIN, ETHANOL AND CYSTEAMINE IN THE RAT
Autore:
PENDLEY CE; FITZPATRICK LR; EWING RW; MOLINO BF; MARTIN GE;
Indirizzi:
RHONE POULENC RORER CENT RES,DEPT PHARMACOL,500 ARCOLA RD,POB 1200 COLLEGEVILLE PA 19426 RHONE POULENC RORER CENT RES,DEPT MED CHEM COLLEGEVILLE PA 19426
Titolo Testata:
The Journal of pharmacology and experimental therapeutics
fascicolo: 3, volume: 265, anno: 1993,
pagine: 1348 - 1354
SICI:
0022-3565(1993)265:3<1348:TGCRAL>2.0.ZU;2-Z
Fonte:
ISI
Lingua:
ENG
Soggetto:
SOMATOSTATIN-CONTAINING CELLS; RABBIT FUNDIC MUCOSA; CCK-B; DUODENAL-ULCER; POTENT; PROPIONITRILE; RANITIDINE; L-364,718; ANTIULCER; PARIETAL;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
34
Recensione:
Indirizzi per estratti:
Citazione:
C.E. Pendley et al., "THE GASTRIN CHOLECYSTOKININ-B RECEPTOR ANTAGONIST L-365,260 REDUCES BASAL ACID-SECRETION AND PREVENTS GASTROINTESTINAL DAMAGE-INDUCED BY ASPIRIN, ETHANOL AND CYSTEAMINE IN THE RAT", The Journal of pharmacology and experimental therapeutics, 265(3), 1993, pp. 1348-1354

Abstract

L-365,260, a nonpeptide antagonist of gastrin/CCK-B receptors, was evaluated in receptor binding, antisecretory and gastrointestinal damageassays. L-365,260 binds potently and stereo-selectively to gastrin and CCK-B sites in guinea pig tissue. In contrast, L-365,260 binds to the isolated canine parietal cell gastrin receptor weakly, and without stereoselectivity. In the pylorus-ligated rat, low doses of L-365,260, given i.v., attenuated pentagastrin-stimulated acid secretion, whereashigher doses were required to inhibit both histamine-stimulated and basal acid secretion. In an aspirin-induced gastric damage model, L-365, 260 was 2.4-fold less potent than the standard histamine H-2 antagonist cimetidine in preventing gastric damage when given i.v., and was 8.3-fold less potent than cimetidine when given p.o. Moreover, the ED50value for L-365,260, given i.v., in prevention of aspirin-induced gastric damage (11.5 mg/kg) agreed well with its ED50 value for inhibition of basal acid secretion (1 2.6 mg/kg). At doses as great as 1 00 mg/kg p.o., neither L-365,260 nor cimetidine had an effect on ethanol-induced gastric damage. L-365,260, although p.o. less bioavailable relative to cimetidine in the aspirin gastric damage model, was as potent ascimetidine in the prevention of cysteamine-induced duodenal ulcers inthe rat. We conclude that the gastrin/CCK-B receptor antagonist L-365,260, at doses supramaximal for the inhibition of pentagastrin-stimulated secretory responses in vivo, inhibits gastrointestinal damage in models of peptic ulcer disease by an antisecretory mechanism of action.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 03/12/20 alle ore 15:49:17