Antisecretory activity

Bismuth Subsalicylate. (2-Hydroxybenzoato-0 )-oxobismuth [14882-18-9] (Pepto-Bismol) maybe made by the process described in Reference 10. Bismuth subsaHcylate has been shown to bind toxins produced by several bacterial strains. It may also act as a result of its saHcylate component on prostaglandin formation and have specific intestinal antisecretory activity. It has been found to be effective in the prevention and therapy of... 

A partially reduced quinoline derivative with antiulcerative and antisecretory activities is isotiquimide (14). It may be synthesized by metallating (with n-BuLi) 4-methyl-5,6,7,8-tetrahy-droquinoline and condensing this with dimethylmethoxysilylisothiocyanate to produce the desired thioamide isotiquimide (14) [4],... 

TURNBERG L A (1983) Antisecretory activity of opiates in vitro and in vivo in man. Scand J Gastroenterol Suppl. 84 79-83. 

The most potent activities (gastric antisecretory activity in the pylorus-ligated rat or anti-ulcer activity on stress-induced gastric lesion in rat) have been observed with compounds (30), (31) [106], (32) [107], (33) and (34) [108], which were shown neither to be histamine H2 receptor inhibitors nor to act as anticholinergic agents. Thus, the activity of compound (32), for example, has been reported to be superior to that of cimetidine [107],... 

The ability of feverfew extract to inhibit 5HT-secretion in platelets was used to identify compounds responsible for the inhibitory effects on platelets [44], A crude feverfew extract was separated by chromatography and fractions were screened for antisecretory activity induced by adrenaline. In five active fractions compounds were identified as the sesquiterpene lactones parthenolide (1), canin (19), artecanin (20), secotanapartholide A (24) and 3 8-hydroxyparthenolide (2). The ability of parthenolide to affect platelet activity induced by other agents was confirmed in a study of direct comparison of crude feverfew extract with parthenolide [43], Parthenolide in the micromolar concentration range inhibited platelet 5HT-secretion. 

Many preparations of feverfew are available to the general public from health food shops and similar outlets in the U.K. They take the form of herbal or homeopathic preparations. The herbal preparations may contain just dried leaf in tablet or capsule form or indeed the dried whole plant. There are many different dosages on the market ranging from 25 to 390 mg per tablet or capsule. When the platelet antisecretory activity that could be extracted from some of these preparations was compared with that extracted from known amounts of feverfew, the apparent feverfew content of most preparations was found to be lower that that stated on the preparation [70]. In the case of the homeopathic preparation, no antisecretory activity was detected. 

Antisecretory activity, 2 Antitussive, 11 Antiulcer activity, 2 Apazone, 475... 

The beneficial effect of fluorine atoms on hydrolytic stability has been demonstrated with synthetic prostaglandin (SC-46275). This compound possesses an antisecretory activity that protects the stomach mucous membrane. However, its clinical development was too problematic because of the instability of the tertiary allyl alcohol function in acidic media (epimerization, dehydration, etc). A fluorine atom has been introduced on the C-16 methyl to inhibit the formation of the allylic carbocation (Figure 4.39). The fluoroanalogue possesses the same biological activity but does not undergo any degradation or rearrangement, and it epimerizes only slowly. 

H6r, M., Heinrich, M., and Rimpler, H., Proanthocyanidin polymers with antisecretory activity and proanthocyanidin oligomers from Guazuma ulmifolia. Phytochemistry, 42, 109, 1996. 

Amino-2,l-benzisothiazoles possess analgesic, antipyretic, tran-quilizing, and muscle-relaxant properties.100-103 The 3-methylamino derivative, in particular, displays potent gastric antisecretory activity.101,129 Diazotization of 3-amino-2,l-benzisothiazoles and coupling with tertiary aromatic amines yield a variety of azo dyes especially suitable for disperse dyeing of synthetic polymer fibers 116,117, n -121.13°. i 1... 

Gallo-Torres et al. (1979) described in detail a method for the bioassay of antisecretory activity in the conscious rat with acute gastric fistula with additional collection of the biliary and pancreatic secretion by means of a catheter in the common bile duct. The gastric secretions are collected by gravity via a cannula in the most gravity dependent site of the glandular stomach. 

Bum JH, Finney DJ, Goodwin LG (eds) (1952) Biological standardization, Chapter XVII, Gastric secretion. Oxford University Press, London, pp 332-334 Gallo-Torres HE, Kuhn D, Witt C (1979) A method for the bioassay of antisecretory activity in the conscious rat with acute gastric fistula Studies with cimetidine, somatostatin, and the prostaglandin E2-analog RO 21-6937. J Pharmacol Meth 2 339-355... 

Beattie DE, Crossley R, Curran ACW, Hill DG, Lawrence AE (1977) 5,6,7,8-Tetrahydro-quinolines. 5. Antiulcer and antisecretory activity of 5,6,7,8-tetrahydroquinolinethioureas and related heterocycles. J Med Chem 20 718-721... 

For their antispasmodic and antisecretory activities in humans, the drugs are administered orally. A comparison of their oral doses (micromoles) indicates that atropine is the most active compound. In clinical experience all three types of anticholinergic activities are exhibited by all compounds. The principal advantage of the available quaternary ammonium compounds lies in the fact that they are elatively free of any of the CNS effects that rm/ be seen with atropine. This may permit the administration of sufficient quantities of the compounds to achieve a more fully effective peripheral anticholinergic action. 

Stoss has reported51 antisecretory activity for sulfoximides (64) derived from l,2-benzothiazin-3-ones. 

In addition to inhibiting HC1 secretion directly by agonist action on the newly discovered PGE receptors (Fig. 13-2), E-type PGs are also cytoprotective to the mucosa. This is independent of the antisecretory activity and may involve increased secretion of alkaline substances (HC03 ) and mucus, which both act synergistically. The gel-like mucus adheres to mucosal cells, giving mechanical protection. It also inhibits the back diffusion of H+, which makes acid neutralization by HC03 easier. Mast cell membrane stabilization by PGs, and possibly other substances, may also occur. 

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