摘要:

AbstractMyometrial tissue was obtained from non‐pregnant women subjected to hysterectomy because of various gynaecological disorders, and from women undergoing caesarean section. Strip preparations were dissected and isometric tension was recorded. Nifedipine (2.9×10‐8‐2.9×10‐6M) inhibited spontaneous contractile activity, mainly by reducing the amplitude of contraction in both non‐pregnant and pregnant myometrium. The drug also inhibited potassium induced contractions in a concentration dependent manner. This effect seemed to be more pronounced in pregnant than in non‐pregnant tissue. In preparations of pregnant human myometrium, normally polarized or potassium depolarized, oxytocin induced a contractile activity that was effectively inhibited by nifedipine. Nifedipine also relaxed contractions induced by vasopressin in isolated non‐pregnant myometrium. It is concluded that the relaxant effect of nifedipine on isolated pregnant and non‐pregnant human myometrium can be explained by inhibition of calcium influx. The results thus support the view, that calcium influx is an important step in the initiation of contractile activity in human uter

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02364.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractSerum concentrations of diazepam and N‐desmethyldiazepam were measured in six adult patients following administration of 10 mg diazepam in solution by the rectal, intravenous, and intramuscular routes. Maximum serum concentrations of 121‐200 ng/ml were recorded from 10 to 20 min. after the rectal instillation, whereas following intramuscular injection the levels rose slowly and irregularly, reaching a maximum (62‐186 ng/ml) in 1 to 24 hours. The bioavailability of diazepam given by rectal instillation was found to be 50±17 per cent (mean±S. D.) as compared with the intravenous administration. The possible reasons for the low bioavailability are discussed. It is concluded that administration by rectal tube provides a useful alternative to the tablets (and intramuscular injections) when a rapid onset of effect of the drug is wanted, and when intravenous administration is not applicable or pr

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02365.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractNaloxone has been accepted as a potent antagonist towards several narcotic analgesics, e.g. morphine, heroin and pethidin. Its effect as an antagonist and its potency against ketobemidone have not been tested in man. We have described the antagonistic effect of naloxone towards the respiratory depression caused by the administration of ketobemidone to patients anaesthetized with N2O/O2and methohexitone.

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02366.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractFluoride concentrations at and above 0.9 mM caused a progressive, concentration‐related inhibition in the incorporation of both14C‐leucine and3H‐thymidine in LS cells incubated in medium with serum. The incorporation of leucine was more affected than that of thymidine, Lowering the pH enhanced the effect of fluoride on both. Removing serum from the incubation medium changed the effect of fluoride, particularly at low pH (7.0). Incorporation of leucine was then stimulated by low fluoride concentrations (0.5 and 0.9 mM), and the effect on thymidine incorporation was eradicated up to 1.3 mM‐NaF. No differences were found in the pool and the specific activity of14C‐leucine in the fluoride exposed cells compared to control cells without fluoride (incubated at pH 7.4 in medium without serum). The cellular pool of3H‐thymidine decreased markedly during the incubation period, somewhat less in the fluoride exposed cells than in

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02367.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractThe antiarrhythmic effects of dl‐propranolol, d‐propranolol, metoprolol and lidocaine against ouabain‐induced cardiac arrhythmias were studied. It was found that contrary to earlier findings in the dog, the effects of the adrenergic β‐blockers against ouabain‐arrhythmias in guinea pigs were due to β‐blocking activity and not the membrane‐stabilizing activity of the compounds. The cardioselective β‐blocker, metoprolol, was more or equally effective as dl‐propranolol against ouabain‐induced arrh

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02368.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractCebus apella monkeys subjected to chronic haloperidol administration develop neurologic disturbances very similar to neuroleptic‐induced acute dystonia in human beings. After varying lengths of time, certain monkeys develop a prolonged dyskinetic syndrome resembling tardive dyskinesia (TD), as seen clinically. Two monkeys with signs of TD were given single intramuscular injections of various compounds with known effects on the catecholaminergic, cholinergic, serotoninergic and GABA‐ergic neurotransmittor systems, and their effect on the TD signs were rated. Dopamine receptor blockers as well as cholinergics had an ameliorating effect on the symptoms. Some compounds known to activate the GABA system, including some benzodiazepines and the GABA‐transaminase inhibitor amino‐oxyacetic acid, also reduced the symptoms, as did the serotonin precursor L‐5HTP. Results with serotonin antagonists were equivocal. It is concluded that dopamine receptor blockade, as well as increased activity within the GABA‐ergic or cholinergic systems cause alleviation of TD. The findings are in agreement with earlier reports in man and thus seem to validate this pr

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02369.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractThe flame retardant tris(2,3‐dibromopropyl)phosphate (Tris‐BP) is converted to products which are mutagenic forSalmonella typhimuriumTA 100 in the presence of rat liver microsomes, NADPH and oxygen. Other bromopropyl‐compounds were also mutagenic; 2,3‐dibromopropene and 2,3‐dibromopropionic acid were directly mutagenic, whereas 2,3‐dibromopropanol and tris(2‐bromopropyl)phosphate were weakly mutagenic after addition of liver microsomes and cofactors. Typicalin vivoandin vitroinhibitors of cytochrome P‐450 inhibited Tris‐BP mutagenicity. The effects of inducers of cytochrome P‐450 on Tris‐BP mutagenicity was dependent on the concentration of mutagen and microsomal protein in the assay, indicating complexity in the kinetics involved when dealing with possible multiple pathways that lead to mutagenicity. Addition of glutathione strongly inhibited Tris‐BP mutagenicity. It is suggested that Tris‐BP is oxidized to a reactive electrophile, possibly the 2‐keto derivative, which could react with nucleophilic groups in DNA and th

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02370.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractMale Wistar rats were given ethanol (approximately 25% of total caloric intake), while two different control groups were pair‐fed isocaloric amounts of lipids or sucrose. After 7‐10 weeks the following organs were studied: liver, cerebrum, heart, diaphragm, kidneys and testes. In fasted, ethanol treated rats there was a reduction in the hepatic concentration of RNA and the cerebral RNA/DNA ratio, when compared tobothcontrol groups, while no effects were found with respect to organ weight and amounts of protein, RNA or DNA in heart, diaphragm, kidneys and testes. When fed, ethanol treated animals were compared tobothcontrol groups, no effects on organ weight and composition were found in any tissue studied. Several significant differences were registered in the ethanol group as compared to one control group only, as well as between the two control groups. The consumption of ethanol (25% of total calories) thus caused only minor alterations in gross organ composition. These results also indicate the importance of interpreting with care any apparent effect of ethanol ingestion, unless at least two different control groups have been emplo

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02371.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractClonidine reduced both the pithed rat heart rate and blood pressure responses to low frequency sympathetic nerve stimulation. Marked shortening of the blood pressure response but not of the heart rate or of the responses to injected noradrenaline was found. This shortening effect was independent of the number of impulses in the train (4‐120 impulses) and of the impulse frequency. It lasted for more than 1 hour and was found to affect only the late part of the pressor decay curve. Nerve stimulations at 2 Hz simulating bursts of different periodicity in the splanchnic nerves showed that the cumulation of the blood pressure between bursts was affected only when these were applied at intervals of more than 10 sec. The effect could not be influenced by antagonists to several known transmitters, by ligation of the renal arteries or by adrenalectomy and does not seem to be mediated by pre‐ or postjunctional a receptor stimulat

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02372.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY

摘要:

AbstractIn isolated human pulmonary arteries and veins the contractile response to noradrenaline (1.8×10‐5M) was 33±7.4% and 20±4.5% (Mean±S. E.M.) of that induced by potassium (127 mM). A variable degree of spontaneous contractile activity was recorded in the vein preparations. This activity was abolished by nifedipine (2.9 × 10‐6M). Digoxin (10‐6M) induced contractions in pulmonary vessels. In the arteries, the digoxin contraction developed slowly and reached a maximum amplitude of 90±4% (Mean±S.E.M.)of the potassium evoked contraction. In the veins, the amplitude of the digoxin contraction was 32±5% of that induced by potassium. Digoxin (10‐6M) also increased the maximum response to noradrenaline and potassium in both arteries and veins. In the arteries, the noradrenaline and potassium contractions increased to 211±6.8% and 145±8.9 of control, and in the veins to 169 ± 13.5% and 163 ± 9.9%, respectively. Nifedipine in concentrations which completely relaxed arterial and venous preparations contracted by potassium, had only a slight relaxing effect on digoxin induced contraction. It is concluded that digoxin increases the tension in pulmonary arteries and veins, and increases the maximum response to noradrenaline and potassium in both types of vessels. The digoxin induced contraction is highly resistant to blockade of extracell

ISSN:0001-6683    

DOI:10.1111/j.1600-0773.1979.tb02373.x

出版商:Blackwell Publishing Ltd    

年代:1979

数据来源: WILEY