摘要:

The plasma levels of unchanged alprenolol and its radioactive metabolites were determined in four healthy male volunteers after intravenous and oral administration of 3H‐alprenolol. The mean plasma half‐life was 2.28 hrs and the apparent volume of distribution 2.99 l/kg as determined from the intravenous experiment. In the rat the tissue distribution was studied after intravenous and oral administration by determination of unchanged drug and its radioactive metabolites, in eight different tissues. A high degree of extra‐vascular distribution of the drug was observed, with especially high amounts of unchanged alprenolol in the lung after intravenous administration. In the rat, dog and man the urinary excretion of total radioactivity after intravenous and oral administration of3H‐alprenolol was studied. It was concluded that the drug was completely absorbed after oral administration. In man, the drug was almost completely excreted in the urine within 48 hrs mainly as metabolites. In the rat and dog a considerable amount of the drug was excreted in the faeces. From studies in the rat and dog it was demonstrated that this was due to biliary excretion of t

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00745.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

The aldehyde dehydrogenases and the drug‐metabolizing system (the mixed function oxidase) were studied in Wistar rats treated with ethanol and phenobarbital. Phenobarbital treatment had no effect on the microsomal aldehyde dehydrogenase activity, whereas the mitochondrial aldehyde dehydro‐genase activity was slightly decreased and the activities of ethylmorphine demethylase, NADPH‐cytochromecreductase and the concentration of cytochrome P‐450 were increased two to threefold. Ethanol treatment caused no changes in the activities of the aldehyde dehydrogenases, and the drug metabolizing system was only slightly affected. Very little aldehyde dehydrogenase activity was found in the cytosol from livers of either control, ethanol‐treated or phenobarbital‐treated rats. The results are discussed with particular reference to the oxidation of acetaldehyde and other aldehydes during ethanol

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00746.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

Adult Wistar rats were injected with Hg‐203 labelled methylmercuric chloride or mercuric chloride. After a methylmercury injection 3‐6 % of the total brain mercury is present in the inorganic form. This represents more inorganic mercury in the brain than after an equal dose of mercuric chloride. The time course of the inorganic mercury content in the brain is dependent on the compound given. Subcellular fractionation shows that the myelin and mito‐chondrial fractions accumulate more inorganic mercury than the other fractions. There is an inverse relationship between the dose of methylmercury given and the amount of inorganic mercury in the

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00747.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

The anaphylactic histamine release from isolated, sensitized rat mast cells was studied. Before incubation the mast cells were kept concentrated (106cells/ml) in either calcium‐free buffer (these cells are denoted Mc) or buffer containing 1 mM‐CaCl2(denoted McCa). The cells were diluted 100 to 400 times when exposed to antigen. The histamine release from Mc and McCa exposed to antigen plus CaCl, was identical, but significantly lower than observed for McCa incubated with antigen alone. EDTA (1 mM) abolished the effect of CaCl2in the incubation medium. Pre‐incubation of McCa in the absence of calcium decreased the response to antigen, and optimal reduction of histamine release was observed within one minute at 37° and five minutes at 21°. The time courses for the anaphylactic histamine release in the presence of calcium from Mc and McCa were identical at both 21° and 37°. The release from McCa in the absence of calcium was considerably faster at both tem

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00748.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

The influence of amphetamine, apomorphine and methylphenidate on basal gastric secretion was investigated using fistula‐ and pylorus‐ligated rats. The antisecretory effect of amphetamine was reversed by pretreating the animals with α‐methyl‐p‐tyrosine (α‐MT). Moreover the decreased output following methylphenidate in shay‐rats was reduced by α‐MT pretreatment. On the other hand α‐MT was not able to antagonize the antisecretory effect of methylphenidate in fistula rats. Apomorphine exhibited antisecretory properties in fistula rats and gastric stimulating effects in shay‐rats, the latter effect being reversed by α‐MT pretreatment. The results obtained indicate that the antisecretory effects of amphetamine and methylphenidate may be due to their

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00749.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

The effect of the following phenoxy herbicides: 2,4‐D, 2,4,5‐T, MCPA, mechlorprop and dichlorprop on the hatchability of hens eggs and the viability of the chicks was investigated both by injecting the herbicides into the yolk and by immersing the eggs in a one or five per cent solution of the herbicides. The five herbicides were found to have rather similar embryotoxic qualities and the injection of about two mg herbicide per 60 g egg decreased the percentage hatch and in some cases the viability of the chicks. Immersion in a one per cent herbicide solution had no effect and immersion in a five per cent herbicide solution had only a moderate effect on the hatchability of the eggs and the viability of the chicks. The embryotoxic effect of 2,7‐dichloro‐dibenzo‐p‐dioxin was found to be at least 100 times that of the herbicides. In the injection experiments a considerable number of malformations was observed in the dead embryos at the high

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00750.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

Seventeen probenecid congeners were tested as inhibitors of the simultaneous uptake of labelled o‐iodohippurate and iodipamide into slices of rabbit renal cortex. Compounds with small substituents on the nitrogen were more inhibitory for o‐iodohippurate, while compounds with larger lipophilic substituents were more inhibitory for iodipamide uptake. The results are interpreted in terms of differential inhibition of two transport systems: the classical hippurate or H‐system and the liver‐like L

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00751.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

A procedure is described by means of which the rates of CO2elimination from small animals, from seeds, or from samples of surviving tissues, can be determined and registered automatically by a strip‐chart recorder. The specimen under study is placed in a closed‐circuit arrangement in which CO2is absorbed in a Sr(OH)2solution. The registration of the CO2liberation is based on the change in the electrical conductivity of the Sr(OH)2solution which occurs during the CO2absorption. The proposed arrangement is suitable for the determination of a quantity of CO2up to 5 μM. When this amount of CO2is liberated in less than one hour, an accuracy of ± 0.5 per cent can easily be obt

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00752.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

In a double‐blind clinical study, a comparison was made of pentazocine, aspirin and placebos, in varying dosage levels, following oral surgery. These were administered orally to 378 patients during the first 24 hours following surgical removal of impacted mandibular third molars. The patients were divided into eight groups which were found to be homogeneous with respect to age, sex, weight and eruptive state of the tooth involved. They were given pentazocine at four dose levels and aspirin and placebos at three dose levels. In all 60 patients had no pain during the 24 hours following surgery. There were no significant differences in between the results among the eight patient groups, with regard to which drug they had received. The majority of patients slept well. However, patients who received aspirin slept significantly better than those receiving pentazocine or placebos. Of 136 patients reporting side effects, there were significantly more complaints from the patients taking pentazocine than from those treated with aspirin or placebo

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00753.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY

摘要:

Four groups of rats were given food containing 0, 40, 70, or 100 mmol LiCl per kg dry weight, respectively. They had free access to water and 0.46 M‐NaCl. This regimen was maintained for one month, and the rats did not develop lithium intoxication in spite of the high lithium dosage. The rats given lithium‐containing food drank more sodium chloride solution than the control rats, and the intake increased with the lithium content of the food. Access to sodium chloride solution was then discontinued. In the two groups given the highest lithium dosages this led within four days to a marked loss of body sodium and a proportionate loss of body weight, a significant decrease of serum sodium, and the development of severe lithium intoxication. Half of the rats in these groups died within 16 days. When rats with severe lithium intoxication were given access to 0.15 M‐NaCl, they drank so much of the sodium chloride solution within one hour that their body weight prior to the intoxication was re‐established. The experiments indicate that administration of lithium leads to a lowered ability of the kidneys to conserve sodium and a consequent increased requirement for sodium. If this is not fulfilled, the animals lose sodium and develop severe lithium intox

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1974.tb00754.x

出版商:Blackwell Publishing Ltd    

年代:1974

数据来源: WILEY