摘要:

AbstractNo experimental data on the regulatory mechanism of the change in vaginal blood flow occuring at sexual arousal exist. Six women Were in a controlled laboratory study given atropine 0.035 mg/kg intravenously. The basal vaginal blood flow was recorded by a heat probe kept at set temperature on the vaginal wall. During sexual stimulation the flow was increased as in women when no drugs are applied and orgasm was unaffected as well. The neurotransmitter has been supposed to be acetylcholine but the present experiments suggest that it is not an atropine sensitive traditional muscarinic transmission. Methylatropine was given in five subjects and neither in these cases any effect on the vaginal vascular response was observed.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02461.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractThe metabolism of the dinitrophenols DNOC and DNBP and their respective monoamino derivatives, 6‐ANOC and 6‐ANBP, was studied in rat caecal incubates. All of the compounds were reduced to their corresponding diamino metabolites. The results are discussed in relation to the comparative toxicology of the dinitrophenols with special regard to a possible significance of the intestinal metaboli

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02462.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractThe pharmacokinetic conditions for oral administration of 5‐fluorouracil (5‐FU) were investigated in 16 patients with malignant liver tumours. The concentration of 5‐FU in portal and systemic blood was determined by a microbiologic method every 10 min. during 2 hours after oral or intravenous administration of a standard dose of 250 mg 5‐FU (∼ 4 mg/kg b.wt.) or 15 mg 5‐FU/kg b.wt. The drug was rapidly absorbed after oral administration with peak values within 10–30 min. 25% of the lower and 40% of the higher oral dose reached the systemic circulation. The reduction of systemic bio‐availability was partly accomplished by a loss in the gastrointestinal tract and partly by extraction by the liver. The hepatic extraction ratio was calculated to 0.56 and 0.26 after the lower and the higher dose respectively indicating a saturable process. The availability of 5‐FU was significantly higher in portal blood than in systemic blood after oral administration. The opposite conditions were found after intravenous administration. Thus, oral administration of 5‐FU to patients with malignant liver tum

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02463.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractThe elimination pattern and tissue distribution in rats of intravenous [14C‐gluconic acid]‐poly(sorbitol‐gluconic acid) and59Fe‐iron‐poly(sorbitol‐gIuconic acid) complex, glusoferron (Ferastral®) have been examined. Twenty‐four hours after injection of 20 or 200 mg/kg of [14C‐gluconic acid]‐poly(sorbitol‐gluconic acid), 5%‐6% of the injected dose of radiolabel was eliminated as14CO2and about 85% in the urine and faeces. Administration of59Fe‐iron‐poly(sorbitol‐gluconic acid) complex (10 and 100 mg of iron/kg) resulted in a urinary and faecal excretion of about 18 % and 40% of the given dose, respectively, during the first 4 days. Biliary excretion was low. The mean molecular weight of the biliary product after the iron complex was lower than that of the parent compound. Radiocarbon in tissues after 24 hours was negligible. Liver and bones accounted for most of the retained radioiron following 100 mg of iron/kg body weight of the59Fe‐iron complex with maximum levels of 27% and 12% of the injected dose, respectively, 4 days after dosing. Red cell incorporation of59Fe attained a leve

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02464.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractThe hepatic cellular distribution in rats of radioiron and radiocarbon after [14C‐gluconic acid] — and59Fe‐labelled iron‐poly(sorbitol‐gluconic acid) complex, glusoferron (Ferastral®), has been investigated. Following administration of the59Fe‐iron complex at a dose level corresponding to 10 mg of iron per kg bodyweight, the ratio of radioactivity per 108cells in parenchymal (P) and non‐parenchymal (NP) cell fractions, the P/NP ratio, was 3.0 after 24 hours and rose to 10.4 at day 14. After 100 mg/kg the ratio was 0.9, 10.5 and 5.7 at day 1,4 and 14, respectively. Radiocarbon content in the different cell compartments fell steadily throughout. Radioiron from59Fe‐iron‐poly(sorbitol‐gluconic acid) complex was shown to be incorporated into whole liver59Fe‐ferritin.In vitrouptake studies with the different liver cells were also performed. Parenchymal cells were found to be more active than non‐parenchymal cells with regard to cellular uptake of radiolabel from both iron complex and polym

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02465.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractMultiple forms of liver microsomal cytochrome P‐450 in rats were identified on SDS‐polyacrylamide gels stained for protein and peroxidase activity after induction with phenobarbital, 3‐methylcholanthrene, and 16α‐cyanopregnenolone. The induced forms were correlated to thein vitrometabolism of biphenyl, benzo(a)pyrene and the steroids 4‐androstene‐3,17‐dione and 5α‐androstane‐3α,17β‐diol. Induction of two forms with apparent molecular weights of 54,000 (RLvMc P‐45054) and 50,000 (RLvMc P‐45 050) was obtained with phenobarbital, induction of RLvMc P‐45055and RLvMc P‐45058with 3‐methylcholanthrene and induction of RLvMc P‐45054with 16α‐cyanopregnenolone. The RLvMc P‐45050was mainly associated with the formation of benzo(a)pyrene‐4,5‐dihydrodiol, and 7α‐hydroxy‐4‐androstene‐3,17‐dione. The RLvMc P‐45055and/or the RLvMc P‐45058was mainly associated with the formation of 2‐ and 3‐hydroxybiphenyl and benzo(a)pyrene‐7,8‐dihydrodiol and RLvMc P‐45054was to some extent associated with the formation of benzo(a)pyrene‐4,5‐dihydrodiol and several metabolites of 5α‐androstane‐3α, 17β‐diol. It is suggested that SDS‐polyacrylamide gel electrophoresis may be a valuable complement to enzyme assays in evaluating eff

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02466.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractThe binding of glucuronides to various liver subfractions and to bovine serum albumin correlated with their molecular weight. Higher molecular weight glucuronides bound more readily. 4‐Methylumbelliferyl‐glucuronide had some of the characteristics of phenolphthaleinglucuronide. Simple phenolic glucuronides were much less retained by various hepatic fractions. Glucuronides were most effectively bound to mitochondrial subfractions. Sulphates of 4‐nitrophenol and phenolphthalein were bound to the same degree to bovine serum albumin and hepatic cytosol despite their different molecular structures and we

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02467.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractTen healthy male students were exposed to m‐xylene alone at concentrations of about 6 and 11.5 μmol/l and given a single dose of alcohol (0.4 and 0.8 g/kg) prior to exposure. The effects of these xylene concentrations and alcohol doses, as well as the combined effects of the two xylene concentrations with the higher alcohol dose on psychophysiological functions, such as body balance and reaction time, were assessed. Xylene alone did not significantly impair these functions, although there was a tendency towards impairment by the exposure to the higher xylene concentration. The impairment caused by alcohol alone was dose‐dependent and exceeded that caused by xylene alone. The deleterious effects of xylene combined with alcohol were usually additive, although antagonism of alcohol effects on body balance by the higher xylene concentration was observed. The effects were pharmacodynamic rather than pharmacokinetic in na

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02468.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractLong‐term lithium treated growing animals given 0.8–2.0 mmol/kg/day had a slightly but significantly faster weight gain than control animals. Greater doses did not give rise to significantly increased weight gain. Body composition, i.e., the percentage of water, fat, ash and “protein” was not affected in the faster growing lithium treated animals. The wet weight and the weight after drying of the stomach (with content) was increased shortly (hours) after the acute administration of lithium. The duration of the effect depended on the dose given. The weight of the large intestine was also increased after a dose of lithium, but only after some days of lithium pretreatment and mainly the wet weight. The effect was small but similar on the small intestine. In long‐term lithium treated rats did the faecal weight and volume increase mainly due to increased water content, but only after some days of lithium

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02469.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY

摘要:

AbstractIt has been suggested that lithium exerts some of its pharmacological actions by inhibition of the membrane‐bound enzyme adenylate cyclase. However, the relationship between the lithium inhibition of adenylate cyclase and the corresponding physiological parameters, e.g. lipolysis, has not been investigated. In the present study it was found that lithium inhibited both the norepinephrine‐induced accumulation of cAMP and release of glycerol in isolated rat fat cells, but only in the lower dose range of norepinephrine. At maximally effective concentrations of norepinephrine, where in the presence of 40 mM of lithium the formation of cAMP was reduced by approximally 40%, lipolysis remained unaffected. The basal content of cAMP and the basal release of glycerol were not inhibited by lithium. In addition to the inhibitory effect of lithium, lithium was found to stimulate the release of glycerol. This stimulatory effect of lithium may be explained by a prevention by lithium of the feedback inhibition by free fatty acids of adenylate cyclase and/or triglyceride lipase, since it could be avoided by increasing the concentration of bovine serum albumin in the incubation medium. It is concluded that lithium by inhibition of hormone‐stimulated adenylate cyclase activity inhibits lipolysis only at submaximal hormone concentrations. This dissociation by lithium of cAMP accumulation and glycerol release may suggest that at least at high concentrations of norepinephrine cAMP‐independent factors are involved in li

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1980.tb02470.x

出版商:Blackwell Publishing Ltd    

年代:1980

数据来源: WILEY