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1,2,3,4,4a,9b-Hexahydro-8,9b-dimethyl-4[3-(4-methyl piperazin-1-yl)propionamido] dibenzofuran-3-one dihydrochloride (RU 20201) is an antitussive compound with a potency comparable to that of codeine. Unlike codeine, RU 20201 is devoid of any apparent CNS effects and does not depress the respiratory system. It has no adverse effect on the gastrointestinal tract no has it any analgesic or anti-inflammatory properties. Only at very high doses was a local anaesthetic effect observed.

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A novel compound, 1,2,3,4,4a,9b-hexahydro-8,9b-dimethyl-4-[3-(4-methylpiperazin-1-yl)propionamido]dibenzofuran-3-one dihydrochloride (RU 20201), has been shown to have comparable antitussive activity to that of codeine phosphate in animal experiments after oral administration. RU 20201 was also shown to have local antitussive activity when given by aerosol. This effect took place immediately. Initial observations suggest that RU 20201 is an antitussive compound that exerts its activity in the lungs, probably by direct inhibition of superficial receptors in the respiratory tract.

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Fasting prior to galactosamine treatment caused a significant modification in the liver damage in both rats and hamsters. Fasting after galactosamine treatment did not affect the course of the liver damage. Liver glycogen levels were significantly lower than normal after either fasting or galactosamine treatment in rats and after galactosamine treatment in hamsters. In rats fasted and treated with galactosamine the liver glycogen content was significantly higher than normal. A 24-h period of fasting did not cause any alteration in liver glycogen levels of hamsters.

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Galactosamine caused changes in the livers of rats that were similar to those seen in human viral hepatitis. In hamsters the changes were characteristic of a typical toxic hepatitis. The response by the liver to galactosamine was very variable in both the rat and the hamster and there was a degree of correlation between the raised transaminase levels and the liver cell damage.

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A novel compound N-(2-hydroxyethyl)-maleopimarimidyl morpholide (RU 18 492), was investigated for its effect against galactosamine induced hepatitis in rats. It was found to be active in reducing both serum transaminase levels and morphological changes due to the hepatotoxin. The protection was shown to be dose related and a significant reduction in liver damage was seen at doses of 50-400 mg/kg p.o. RU 18 492 was ineffective against carbon tetrachloride induced hepatitis in rats. It was suggested that the protective effect of RU 18 492 was due to its ability to stimulate the smooth endoplasmic reticulum thus inducing a more rapid detoxification of galactosamine.

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Four compounds, prednisolone, sodium phenobarbitone, azathioprine and orotic acid, were tested for their ability to inhibit galactosamine induced hepatitis in the rat. Prednisolone offered total protection at doses of 100 mg/kg and above; sodium phenobarbitone and orotic acid modified the response to galactosamine and azathioprine was without effect.

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An examination of the hepatotoxicity of d-galactosamine has been made in the golden hamster and the mouse and the results compared to those previously investigated in the rat. The order of species found susceptible to the hepatotoxic effects of d-galactosamine was golden hamster greater than rat greater than mouse.

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1. The effect of d-galactosamine hydrochloride on the livers of rats was observed by measuring serum transaminase levels and histological examination. 2. Galactosamine caused dose related liver cell damage when given i.p. and s.c. but was ineffective when given orally. 3. The time of maximum effect was 24--48 h after administration. 4. The liver cell damage was modified by the oestrus cycle in female rats. 5. Galactosamine when given in proportion to body weight tended to be less effective as body weight increased.

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1. A novel phthalazine analogue taloximine (1-hydroxyimino-4(2-dimethyl-aminoethoxy)-1,2-dihydrophthalazine monohydrochloride monohydrate) stimulated respiration in conscious rabbits at doses of 7 mg/kg and above.2. Taloximine antagonized the depressant action of morphine on respiration in rabbits at doses of 10 mg/kg. At high doses it resuscitated rabbits after they had been given lethal doses of sodium pentobarbitone.3. In in vitro preparations of the trachea or bronchus taloximine was about equiactive with aminophylline. In the Konzett-Rössler preparation the intravenous ED50 for taloximine was about 18% of that of aminophylline, whereas after oral administration the two drugs were equiactive.4. Taloximine, unlike aminophylline, did not protect guinea-pigs against anaphylactic microshock to egg albumen.5. Taloximine shortened the duration of the loss of righting reflex in mice due to hexobarbitone more effectively than bemegride, nikethamide or vanillic acid diethylamide.6. In the dose required to stimulate respiration taloximine had only slight cardiovascular effects. Up to four times this dose produced no evidence of general excitation of the central nervous system.

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