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Query: UMLS:C0038358 (gastric ulcer)
 5,179 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Effects of (-) cis-2,3-dihydro-3-(4-methylpiperazinylmethyl)-2-phenyl-1,5-benz othiazepin-4-(5H ) -one hydrochloride (BTM-1086) on various experimental gastric and duodenal ulcers were studied in rats. In the pylorus-ligated ulcer, restraint and water immersion stress ulcer, and drug-induced ulcer (indomethacin, aspirin, reserpine, serotonin, cysteamine), BTM-1086 prevented the development of ulcer at a dose of 0.1 to 1 mg/kg, p.o., but only weakly inhibited the histamine-induced gastric ulcer. The inhibitory activities of BTM-1086 were significantly higher than those of atropine sulfate. In the healing experiment with the acetic acid-induced stomach ulcer, BTM-1086 (1 mg/kg/day, p.o., X 14) showed a significant healing effect, which was higher than that of propantheline bromide. BTM-1086 at a dose of 0.2 mg/kg, i.d., remarkably inhibited the gastric secretion 6 hr after pylorus ligation. The aspirin-induced reductions of the total acid and K+ as well as the increments of the volume and Na+ in the gastric secretion were prevented dose-dependently by pretreatment with BTM-1086.
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PMID:Antiulcer effect of (-)-cis-2,3-dihydro-3-(4-methylpiperazinylmethyl) -2-phenyl-1,5-benzothiazepin-4-(5H)-one hydrochloride (BTM-1086) in experimental animals. 376 47

6-[1S-(3S,4-Dihydro-8- hydroxy-1H-2-benzo-pyran-1-one-3-yl)- methylbutylamino]-4S,5S-dihydroxy-6-oxo-3S-ammoniohexanoate (AI-77B)-gamma-lactone-N-ethyl derivative (AI-77-C2) is a new antiinflammatory drug with antiulcer activity. In the first part of the present study the ulcerogenicity of this drug was assessed. Acidic antiinflammatory drugs--indomethacin and diclofenac--and basic antiinflammatory drugs--tiaramide and mepirizole--were used for comparison. Although AI-77-C2 was barely ulcerogenic at 7 h after dosing, some lesions developed in both stomach and intestine at 24 h. Repeated administrations over 5 days appeared to increase its ulcerogenicity and general toxicity. Marked gastric ulcers were induced by indomethacin and diclofenac, and severe intestinal ulcers were also produced at 24 h and by their repeated administration. Tiaramide did not induce marked ulcers in any case. Although the ulcerogenicity of mepirizole was weak at 7 h, severe duodenal ulcers developed at 24 h and after the repeated administration. From the results given above, it was concluded that the ulcerogenicity of AI-77-C2 was relatively low. In the next study, the antiulcer activity of AI-77-C2 was examined in several experimental ulcer models. AI-77-C2 showed a marked inhibition of all the models presently employed, i.e., the indomethacin-induced gastric ulcer, the pylorus ligation ulcer, the water immersion stress ulcer, and the acetylsalicylic acid-induced ulcer in rats. It was observed that AI-77-C2 suppressed the gastric secretion and movement. It is therefore concluded that the antiinflammatory drug AI-77-C2 has low ulcerogenicity and potent antiulcer activity.(ABSTRACT TRUNCATED AT 250 WORDS)
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PMID:Ulcerogenic and antiulcerogenic effects of a new antiinflammatory drug, the gamma-lactone-N-ethyl derivative of 6-[1S-(3S,4-dihydro-8-hydroxy-1H-2-benzo- pyran-1-one-3-yl)-3-methylbutylamino]-4S,5S-dihydroxy-6-oxo-3S- ammoniohexanoate, on gastrointestinal tract in rats. 379 Jan 91

Methylphenidate (5, 10, or 20 mg/kg/day) or saline were administered to rats in the activity-stress ulcer paradigm. Running-wheel activity and food consumption did not differ among groups. Methylphenidate produced dose-related increases in gastric ulcer severity, decreases in hypothalamic noradrenaline (NA) and increases in 3-methoxy-4-hydroxy-phenylethyleneglycol sulfate (MHPG-SO4) in the hypothalamus, amygdala, hippocampus and thalamus. These results differ markedly from the effects seen with a related substance, d-amphetamine, and suggest different mechanisms of action for these drugs.
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PMID:Methylphenidate effects on activity-stress gastric lesions and regional brain noradrenaline metabolism in rats. 404 33

The effects of 5-acetylspiro[benzofuran-2(3H),1'-cyclopropan]-3-one (AG 629), a newly synthesized compound, on various experimentally induced ulcers were investigated. Oral or intraduodenal administration of AG 629 in a dose range of 25-100 mg/kg inhibited water-immersion stress ulcer, exertion ulcer, Shay ulcer, indometacin- and acetylsalicylic acid (ASA)-induced gastric ulcer, and indomethacin-induced small intestinal ulcer in rats, histamine-induced gastric ulcer in guinea pigs, and ASA-induced gastric ulcer in dogs, though it was not effective against cysteamine-induced duodenal ulcer in rats. AG 629 in doses of 6.3-25 mg/kg p.o. twice a day significantly promoted the healing of acetic acid- or thermal-cortisone-induced gastric ulcers and acetic acid-induced duodenal ulcers in rats. AG 629 (25-100 mg/kg i.d.) inhibited the secretion of gastric acid and pepsin in pylorus-ligated rats and the acid secretion stimulated by distension of the rat stomach with air, whereas this compound did not affect acid secretion stimulated by histamine, pentagastrin, carbachol or 2-deoxy-D-glucose. This study shows that AG 629 has both prophylactic and curative effects on various ulcers. The anti-ulcer effect of this agent seems to be mediated primarily by increasing mucosal resistance and secondarily by an antisecretory activity.
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PMID:Effects of 5-acetylspiro[benzofuran-2(3H),1'-cyclopropan]-3-one, a new anti-ulcer agent, on experimental acute and chronic ulcers. 407 15

Several sulfhydryl substances were found to protect the gastric mucosa against the ulcerogenic effect of indomethacin, while being ulcerogenic in stress (restraint) ulcer. D-penicillamine showed a dose dependent antiulcerogenic effect in both gastric ulcer models. This experimental result has called attention to the two methyl groups in which the D-penicillamine molecule was different from D-cysteine. It seemed therefore that in contrast to cysteine the favourable effect of D-penicillamine in stress ulcer, was due to this structural difference.
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PMID:The effect of D-penicillamine in different experimental gastric ulcer models in the rat. 409 42

Mild stress of restraint for 10 min at an ambient temperature of 18 degrees C increased serum corticosterone levels in rats considerably. Histamine given intravenously prior to restraint alone significantly further intensified the stress-induced elevation of serum corticosterone. Dimaprit and cimetidine failed to modify corticosterone responses to the mild stress. Severe stress of restraint and cold of 3 h duration increased serum corticosterone and free fatty acid levels considerably. Histamine given prior to stress exposure left the corticosterone and hyperlipaemic responses to severe stress unchanged. Dimaprit inhibited and cimetidine intensified the stress-induced hyperlipaemia. The most striking finding in the present experiment was a powerful inhibition of gastric stress ulcer generation by intraventricularly administered histamine. Dimaprit was similarly effective. This strong anti-ulcer effect of histamine was abolished by intraventricular pretreatment of rats with either H1- or H2-receptor antagonists, chloropyramine or cimetidine. The results may suggest that in the rat a mild stress does not fully activate central histaminergic pathways involved in corticosterone responses. During severe stress histamine considerably prevents gastric ulcer generation and both H1- and H2-receptors mediate this action of histamine.
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PMID:The involvement of central histamine receptors in stress-induced responses of serum corticosterone and free fatty acids and in gastric ulcer development. 611 42

Gastric mucosal defensive factor plays an important role in the pathogenesis of various gastric diseases as well as aggressive factor such as acid. Gastric mucosal defensive factor of various gastric diseases and the relation to acid secretion were studied. The influence of operative insult and obstructive jaundice on gastric aggressive and defensive factors was also studied. Defensive factor was investigated using gastric transmucosal potential difference (PD). The results obtained were as follows: PD showed low value in the gastric diseases with the mucosal lesion such as gastric ulcer, stress ulcer and bleeding gastric ulcer. Particularly the last two diseases, which had active mucosal bleeding, showed remarkably low values. PD tended to increase following acid secretion but had no significance. Operative insult seemed to cause transient increase of intragastric pH and deterioration of gastric defensive factor, and the change was enhanced by obstructive jaundice.
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PMID:[Gastric mucosal defensive factor in various gastric diseases--with special reference to the influence of the operative insult and obstructive jaundice]. 647 52

The erythro version of 1, 4,-dimercapto-2, 3,-butanediol provided a significant protection against experimental gastric ulcer induced by indomethacin, while it was ineffective in stress ulcer of rats. The threo version of the same compound showed a complete ineffectiveness. It seems that most probably there is a specific receptor system in the living organism where only the erythro version is effective. Moreover, there was a remarkable difference between indomethacin-induced and stress ulcer as far as their protection is concerned. Sulfhydryl containing substances inhibited indomethacin ulcer but they were ineffective against stress ulcer. This experimental result provides further data for the difference of the pathomechanism of various experimental ulcers and thus their direct extrapolation to the human disease and to its treatment needs extreme caution.
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PMID:Different protective effects of dimercapto-butanediol stereoisomers in experimental gastric ulceration. 665 99

Prognostic indicator for acute gastric ulceration was experimentally investigated using water immersed and restrained rats, with special interest in influence of obstructive jaundice and effect of vagotomy. The results obtained are as follows: Intragastric pH and gastric mucosal potential difference (PD) faithfully reflected the ulcer index. This shows that continuous monitoring of these two parameters may be of clinical use as indicator for acute gastric ulceration in critically ill or postoperative patients. Water immersing and restraint stress ulcer may be caused by imbalance between gastric offensive and defensive factors as a result of progressively increasing gastric secretion and progressively deteriorating gastric mucosal barrier. Gastric ulceration was enhanced in rats with obstructive jaundice, probably because of compromised defensive factor. Prophylaxis of acute gastric ulceration with or without obstructive jaundice may not be attained by vagotomy alone; an adequate maintenance of defensive factor seems to be also necessary.
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PMID:[Experimental study on acute gastric ulceration in rat--including influence of obstructive jaundice and vagotomy]. 667 85

The pathophysiology of clinical peptic ulcer, which is diverse for duodenal, chronic gastric or stress ulcer in humans, has been only partially elucidated by experimental animal studies. A central role of vascular disturbance and acid back diffusion for human stress and animal stress ulcers is evident, whereas a complex and variable set of functional disorders may relate to duodenal ulcer, though the role of acid is paramount. Mucosal resistance factors are of major importance in all types of ulcer and are of particular interest in chronic gastric ulcer. The importance of selecting, for anti-ulcer drug testing, appropriate ulcer models is emphasized, and more extensive use of chronic experimental ulcer healing rate changes, mucus glycoprotein analysis, and cytoprotective changes is recommended. Novel compounds such as pirenzepine, which act on some muscarinic receptors, will help elucidate ulcer pathophysiology as well as provide medical therapy, particularly since all postganglionic vagal transmitter substances in gastric or duodenal mucosae have not yet been identified.
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PMID:Experimental studies on the pathophysiology of peptic ulcer disease. 675 13


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